| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| BIBR 1532 | Axon 2301
CAS [321674-73-1]
MF C21H17NO3MW 331.36
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of native and recombinant human telomerase (IC50 values of ca. 100 nM), capable of inducing senescence in human cancer cells. BIBR1532 is a mixed-type non-competitive inhibitor of the human telomerase reverse transcriptase and human telomerase RNA components with similar potency primarily by interfering with the processivity of the enzyme. BIBR 1532 defines a novel class of mixed-type non-competitive telomerase inhibitor with mechanistic similarities to non-nucleosidic inhibitors of HIV1 reverse transcriptase.
References
Certificates
Categories
Extra info
E. Pascolo et al. Mechanism of human telomerase inhibition by BIBR1532, a synthetic, non-nucleosidic drug candidate. J. Biol. Chem. 2002, 277, 15566-15572.
D.K. Barma et al. Inhibition of telomerase by BIBR 1532 and related analogues. Bioorg. Med. Chem. Lett. 2003, 13, 1333-1336.
K. Damm et al. A highly selective telomerase inhibitor limiting human cancer cell proliferation. E.M.B.O.J. 2001, 20, 6958-6968.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
RT
p53-Tumor Suppression
DNA-damage Response
EC 2.7.7.49
Telomerase
Potent and selective telomerase inhibitor inducing senescence in human cancer cells.
Chemical name
(E)-2-(3-(Naphthalen-2-yl)but-2-enamido)benzoic acid
Parent CAS No.
[321674-73-1]
Order
Size
Unit Price
Stock
5 mg
€70.00
In Stock | | axonmedchem |
| Vercirnon - GSK-1605786 | CCX282-B | Traficet-EN | Axon 2685
CAS [698394-73-9]
MF C22H21ClN2O4SMW 444.93
Purity:
100%
Soluble in DMSO
Description
Vercirnon is an orally bioavailable selective antagonist of the CCR9 chemokine receptor (IC50 values 5.4 nM and 3.4 nM for CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells, respectively). Based on studies of the crystal structure, vercirnon binds to the intracellular side of the receptor, exerting allosteric antagonism and preventing G-protein coupling. Vercirnon was developed for treatment of inflammatory bowel disease, including Crohn's disease and celiac disease.
KEYWORDS: Vercirnon | supplier | CCR9 antagonist | GSK-1605786 | CCX282-B | Traficet-EN | GSK1605786 | GSK 1605786 | CCX282B | CCX282 B | Traficet EN | CAS [698394-73-9] | Chemokine | Chemokine | Antagonist | Receptors | Coeliac disease | Crohn's disease | Coeliac | Crohn | | axonmedchem |
| AMD 3465 hexahydrobromide | Axon 1930
CAS [185991-07-5]
MF C24H38N6.6HBrMW 896.07
Purity:
98%
Soluble in water and DMSO
Description
Potent and selective CXCR4 antagonist; Potent anti-HIV agent that specifically blocks the interaction of HIV gp120 with CXCR4. Compared to AMD 3100 (Axon 1738), AMD3465 was even 10-fold more effective as a CXCR4 antagonist, while showing no interaction whatsoever with CCR5; AMD3465 has the potential to mobilize hematopoietic stem cells
References
Certificates
Categories
Extra info
S Hatse et al. AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor. Biochem. Pharmacol. 2005, 70(5), 752-761.
MM Rosenkilde et al. Molecular mechanism of action of monocyclam versus bicyclam non-peptide antagonists of the CXCR4 chemokine receptor. J. Biol. Chem. 2007, 282, 27354.
V Bodart et al. Pharmacology of AMD3465: a small molecule antagonist of the chemokine receptor CXCR4. Biochem. Pharmacol. 2009, 78(8), 993-1000.
GJ Bridger et al. Synthesis and structure-activity relationships of azamacrocyclic C-X-C chemokine receptor 4 antagonists: analogues containing a single azamacrocyclic ring are potent inhibitors of (...). J. Med. Chem. 2010, 53(3), 1250-1260.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
A2
Chemokine
Potent and selective CXCR4 antagonist
Chemical name
N-(4-((1,4,8,11-tetraazacyclotetradecan-1-yl)methyl)benzyl)-1-(pyridin-2-yl)methanamine hexahydrobromide
Parent CAS No.
[185991-24-6]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| Delavirdine - U 90152 | Rescriptor | Axon 1815
CAS [136817-59-9]
MF C22H28N6O3SMW 456.56
Purity:
99%
Moderately soluble in DMSO
Description
Non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1); Selectively inhibits HIV-1 reverse transcriptase (RNA-dependent DNA polymerase) over other cellular polymerases; Inhibitor of cytochrome P450 isozyme CYP3A4; Interacts with many medications
References
Certificates
Categories
Extra info
PJ Pagano and KT Chong. In vitro inhibition of human immunodeficiency virus type 1 by a combination of delavirdine (U-90152) with protease inhibitor U-75875 or interferon-alpha. J Infect Dis. 1995, 171(1), 61-67.
LJ Scott, CM Perry. Delavirdine: a review of its use in HIV infection. Drugs. 2000, 60(6), 1411-1444.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
RT
p53-Tumor Suppression
DNA-damage Response
EC 2.7.7.49
Cytochrome P450
NNRT inhibitor (HIV-1)
Chemical name
N-(2-(4-(3-(isopropylamino)pyridin-2-yl)piperazine-1-carbonyl)-1H-indol-5-yl)methanesulfonamide
Parent CAS No.
[136817-59-9]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| CP 31398 | Axon 2879
CAS [1217195-61-3]
MF C22H28Cl2N4OMW 435.39
Purity:
98%
Soluble in water and DMSO
Description
CP 31398 stabilizes the core domain of the tumour suppressor p53 in vitro and is an effective anti-cancer drug by virtue of rescuing destabilized mutants of p53. Moreover, CP 31398 can induce apoptosis of human cancer cells.
KEYWORDS: CP 31398 | supplier | p53 stabilizer | CP31398 | CP-31398 | CAS [1217195-61-3] | [259199-65-0] | Non Selective | p53 | Stabilizer | Transcription Factors | Apoptosis | | axonmedchem |
| NSC 348884 | Axon 1402
CAS [81624-55-7]
MF C38H40N10MW 636.79
Purity:
100%
Moderately soluble in DMSO
Description
A putative small molecule inhibitor of nucleophosmin (NPM). NSC 348884 inhibits NPM oligomer formation, up-regulates p53, induces apoptosis and synergizes with chemotherapy
References
Certificates
Categories
Extra info
W Qi et al. NSC348884, a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis in human cancer cells. Oncogene 2008, 27(30), 4210-4220.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
p53
Transcription Factors
p53-Tumor Suppression
DNA-damage Response
Phosphoprotein
NPM
NPM inhibitor
Chemical name
N,N,N',N'-Tetrakis-(5-methyl-1H-benzoimidazol-2-ylmethyl)-ethane-1,2-diamine
Parent CAS No.
[81624-55-7]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| CXCR3 Antagonist 6c - Compound 6c | Axon 1800
CAS [870998-13-3]
MF C30H32Cl3N5O3MW 616.97
Purity:
99%
Soluble in DMSO
Description
Potent chemokine CXCR3 antagonist, exhibiting IC50 value of 60 nM in a calcium mobilization functional assay; dose-dependently inhibiting CXCR3 functional response to CXCL11 as measured by T-cell chemotaxis, with a potency of about 100 nM
References
Certificates
Categories
Extra info
AG Cole et al. Identification and initial evaluation of 4-N-aryl-[1,4]diazepane ureas as potent CXCR3 antagonists. Bioorg. Med. Chem. Let. 2006, 16(1), 200-203.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
A1
Chemokine
CXCR3 antagonist
Chemical name
4-(2-(3-chlorobenzamido)-4-(2,4-dichlorophenethylcarbamoyl)phenyl)-N-ethyl-1,4-diazepane-1-carboxamide
Parent CAS No.
[870998-13-3]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| COTI-2 | Axon 2841
CAS [1039455-84-9]
MF C19H22N6SMW 366.48
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
COTI-2 is an anti-cancer drug which appears to act both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. Proposed to cause cancer cell death via apoptosis. COTI-2 exhibits potent anti-proliferative activity against a wide variety of human cancer cell lines in vitro (at nanomolar concentrations) and against human tumor xenografts.
KEYWORDS: COTI-2 | supplier | p53 activator | COTI2 | COTI 2 | CAS [1039455-84-9] | DNA-RNA | p53 | Activator | Transcription Factors | | axonmedchem |
| Compound 120 - Atazanavir, deuterated | CTP 518 | Axon 1753
CAS [N.A.]
MF C38H37D15N6O7.H2O4SMW 818.03
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
A partially dueterated analog of Atazanavir (Axon 1441), an oral HIV protease inhibitor; A deuterium-containing medicine with improved ADME properties; Compound 120 showed an approximately 50% increase in half life compared with Atazanavir.
References
Certificates
Categories
Extra info
SL Harbeson et al. Azapeptide derivatives. Patent Concert Pharmaceuticals Inc. WO2008156632 (A1)
Certificate of Analysis
Material Safety Data Sheet
Immunology
Non Selective
EC 3.4.23.16
Deuterated Protease inhibitor (see Axon 1441)
Chemical name
(3S,8S,9S,12S)-3-(1,1-dimethylethyl)-12-[1,1-di(methyl-d3)ethyl-2,2,2-d3]-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-2,5,6,10,13-Pentaazatetradecanedioic acid, 1,14-di(methyl-d3) ester sulfate
Parent CAS No.
[1092540-56-1]
Order
Size
Unit Price
Stock
2 mg
€115.00
In Stock | | axonmedchem |
| PF 04981517 - CYP3cide | PF 4981517 | Axon 2026
CAS [1390637-82-7]
MF C26H32N8MW 456.59
Purity:
98%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and selective inhibitor of Cytochrome P450 3A4 (CYP3A4) with IC50 value of 30 nM; inactivates human CYP3A4 in an efficient and time-dependent manner
References
Certificates
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Extra info
RL Walksky et al. Selective mechanism-based inactivation of CYP3A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of CYP3A4 versus CYP3A5 in (...). Drug Metab. Dispos. 2012, 40(9), 1686-1697.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
EC 1.14.13.97
Cytochrome P450
Pfizer Licensed Products
Inhibitor of Cytochrome P450 3A4 (CYP3A4)
Chemical name
(S)-1-methyl-3-(1-methyl-5-p-tolyl-1H-pyrazol-4-yl)-4-(3-(piperidin-1-yl)pyrrolidin-1-yl)-1H-pyrazolo[3,4-d]pyrimidine
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[1390637-82-7]
Order
Size
Unit Price
Stock
10 mg
€110.00
In Stock | | axonmedchem |
| Sulfaphenazole - Depocid | Depotsulfonamide | Plisulfan | Raziosulfa | Axon 2922
CAS [526-08-9]
MF C15H14N4O2SMW 314.36
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Sulfaphenazole is a potent and very selective inhibitor for CYP2C9 with a Ki value between 0.11 and 0.7 μM. Antibiotic.
KEYWORDS: Sulfaphenazole | supplier | CYP2C9 inhibitor | Depocid | Depotsulfonamide | Plisulfan | Raziosulfa | CAS [526-08-9] | CAS [902-02-3] | Non Selective | Cytochrome P450 | Inhibitor | Enzymes | Antibiotic | | axonmedchem |
| WZ 811 | Axon 1620
CAS [55778-02-4]
MF C18H18N4MW 290.36
Purity:
99%
Soluble in DMSO
Description
Potent chemokine CXCR4 receptor antagonist (EC50: 0.3 nM)
References
Certificates
Categories
Extra info
W Zhan et al. Discovery of small molecule CXCR4 antagonists. J. Med. Chem. 2007, 50, 5655-5664.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
A2
Chemokine
CXCR4 antagonist
Chemical name
N,N'-(1,4-phenylenebis(methylene))dipyridin-2-amine
Parent CAS No.
[55778-02-4]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| Exemestane - Aromasin | FCE 24304 | Axon 2045
CAS [107868-30-4]
MF C20H24O2MW 296.40
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO and Ethanol
Description
Orally active, irreversible steroidal aromatase inhibitor (IC50 = 20 nM). Destabilizes aromatase and lowers estrogen levels; breast cancer therapy.
References
Certificates
Categories
Extra info
D Giudici et al. 6-Methylenandrosta-1,4-diene-3,17-dione (FCE 24304): A new irreversible aromatase inhibitor. J. Steroid Biochem. 1988, 30 (1–6), 391–394.
N Mauras et al. Pharmacokinetics and Dose Finding of a Potent Aromatase Inhibitor, Aromasin (Exemestane), in Young Males. J. Clin. Endocrinol. Metab. 2003, 88(12), 5951–5956.
RC Coombes et al. A Randomized Trial of Exemestane after Two to Three Years of Tamoxifen Therapy in Postmenopausal Women with Primary Breast Cancer. N. Engl. J. Med. 2004, 350, 1081-1092.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Endocrinology
EC 1.14.14.1
Cytochrome P450
Pfizer Licensed Products
Irreversible steroidal aromatase (CYP19A1) inhibitor
Chemical name
(8R,9S,10R,13S,14S)-10,13-dimethyl-6-methylene-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[107868-30-4]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| TAK 700 - Orteronel | Axon 2124
CAS [566939-85-3]
MF C18H17N3O2MW 307.35
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent, orally available, and highly selective inhibitor of 17,20-lyase (CYP17A1; IC50 value 19 nM and 48 nM for human and rat respectively) and of correlated androgen synthesis. TAK 700 exhibits no affinity for CYP11B 1and CYP3A4 (IC50 values >1000 nM and >10000 nM resp.), nor for other isoforms of the human CYP enzyme (IC50 values >14000 nM). When given orally to monkeys at a dose of 1 mg/kg, TAK 700 markedly reduced serum testosterone and DHEA at 5 h after administration.
TAK 700 was selected for evaluation in patients in phase III clinical trials for the potential treatment of prostate cancer.
References
Certificates
Categories
Extra info
T. Kaku et al. Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancer. Bioorg. Med. Chem. 2011, 19(21), 6383-99.
M. Yamaoka et al. Orteronel (TAK-700), a novel non-steroidal 17,20-lyase inhibitor: effects on steroid synthesis in human and monkey adrenal cells and serum steroid levels in cynomolgus monkeys. J. Steroid Biochem. Mol. Biol. 2012, 129, 115-128.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Endocrinology
EC 1.14.99.9
Cytochrome P450
Potent and highly selective inhibitor of 17,20-lyase (CYP17A1)
Chemical name
(S)-6-(7-hydroxy-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-7-yl)-N-methyl-2-naphthamide
Parent CAS No.
[566939-85-3]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| Daclatasvir dihydrochloride - BMS 790052 dihydrochloride | Axon 2093
CAS [1009119-65-6]
MF C40H50N8O6.2HClMW 811.80
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent hepatitis C virus (HCV) NS5A protein inhibitor with picomolar EC50 value
References
Certificates
Categories
Extra info
M Gao et al. Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect. Nature 2010, 465, 96–100.
Certificate of Analysis
Material Safety Data Sheet
Immunology
Miscellaneous
HCV NS5A Serine Protease
EC 3.4.21.113
Hepatitis C virus (HCV) NS5A protein inhibitor
Chemical name
Dimethyl (2S,2'S)-1,1'-((2S,2'S)-2,2'-(5,5'-(biphenyl-4,4'-diyl)bis(1H-imidazole-5,2-diyl))bis(pyrrolidine-2,1-diyl))bis(3-methyl-1-oxobutane-2,1-diyl)dicarbamate dihydrochloride
Parent CAS No.
[1009119-64-5]
Order
Size
Unit Price
Stock
2 mg
€85.00
In Stock | | axonmedchem |
| Fluconazole - UK 49858 | Axon 2105
CAS [86386-73-4]
MF C13H12F2N6OMW 306.27
Purity:
99%
Soluble in DMSO
Description
Antifungal agent that inhibits the fungal cytochrome P450 enzyme 14α-demethylase; marketed under the trade names Diflucan and Trican
References
Certificates
Categories
Extra info
JL Goodman et al. A controlled trial of fluconazole to prevent fungal infections in patients undergoing bone marrow transplantation. N. Engl. J. Med. 1992, 326(13), 845-851.
MS Saag, WE Dismukes. Azole antifungal agents: emphasis on new triazoles. Antimicrob. Agents Chemother. 1988, 32(1), 1-8.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Immunology
EC 1.14.13.70
Cytochrome P450
Pfizer Licensed Products
Fungal CYP450 enzyme 14α-demethylase inhibitor
Chemical name
2-(2,4-difluorophenyl)-1,3-di(1H-1,2,4-triazol-1-yl)propan-2-ol
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[86386-73-4]
Order
Size
Unit Price
Stock
50 mg
€60.00
In Stock | | axonmedchem |
| SRPIN 340 | Axon 2200
CAS [218156-96-8]
MF C18H18F3N3OMW 349.35
Purity:
99%
Soluble in DMSO
Description
Selective ATP-competitive inhibitor of SRPK kinase activity (Ki 0.89 μM for SRPK1; 99.2% inhibition of RS-repeat peptide substrate phosphorylation at 10μM). SRPIN340 does not inhibit other classes of Serine-Arginine-Rich Protein Kinases (SRPKs) significantly, including Clk1 and Clk4 and >140 other SR kinases. SRPIN 340 promotes SRp75 degradation, and dose dependently suppressed HCV 1b and 2a replication (EC50 values of 4.7 μM and 15.8 μM resp.) and propagation of Sindbis and HCV-JFH1 viruses in cell culture.
References
Certificates
Categories
Extra info
Y. Karakama et al. Inhibition of Hepatitis C Virus Replication by a Specific Inhibitor of Serine-Arginine-Rich Protein Kinase. Antimicrob. Agents Chemother. 2010, 54, 3179-3186.
T. Fukuhara et al. Utilization of host SR protein kinases and RNA-splicing machinery during viral replication. PNAS USA. 2006, 103, 11329-11333.
S. Oltean et al. SRPK1 inhibition in vivo: modulation of VEGF splicing and potential treatment for multiple diseases. Biochem. Soc. Trans. 2012, 40, 831–835.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
Immunology
SRPK
PI3K-Akt-mTOR
EC 2.7.11.1
Selective ATP-competitive inhibitor of SRPK kinase activity
Chemical name
N-(2-(piperidin-1-yl)-5-(trifluoromethyl)phenyl)isonicotinamide
Parent CAS No.
[218156-96-8]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| ARN 509 - Apalutamide | JNJ-56021927 | Axon 1979
CAS [956104-40-8]
MF C21H15F4N5O2SMW 477.43
Purity:
99%
Soluble in DMSO
Description
A competitive and potent antagonist of androgen receptor (AR); a promising therapeutic in both castration-sensitive and castration-resistant forms of prostate cancer (CSPC & CRPC).
KEYWORDS: ARN 509 | supplier | Androgen antagonist | Apalutamide | JNJ-56021927 | ARN509 | ARN-509 | JNJ56021927 | JNJ 56021927 | CAS [956104-40-8] | Androgenic Hormones | Androgen (AR) | Antagonist | Receptors | | axonmedchem |
| TG 003 | Axon 1765
CAS [719277-26-6]
MF C13H15NO2SMW 249.33
Purity:
98%
Soluble in DMSO
Description
Potent and specific inhibitor of Cdc2-like kinase (Clk) family (Ki = 10 nM for mClk1/Sty; IC50 = 15 nM, 20 nM, 200 nM, and > 10 mM for mClk4, mClk1, mClk2, and mClk3, respectively); a valuable tool to dissect the regulatory mechanisms involving serine/arginine-rich protein phosphorylation signaling pathways in vivo, and potential for the therapeutic manipulation of abnormal splicing
References
Certificates
Categories
Extra info
M Muraki et al. Manipulation of alternative splicing by a newly developed inhibitor of Clks. J Biol Chem. 2004, 279(23), 24246-24254.
A Nishida et al. Chemical treatment enhances skipping of a mutated exon in the dystrophin gene. Nature Commun. 2011, 2, 308.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
EC 2.7.12.1
CLK
Inhibitor of Cdc2-like kinase (Clk) family
Chemical name
(Z)-1-(3-ethyl-5-methoxybenzo[d]thiazol-2(3H)-ylidene)propan-2-one
Parent CAS No.
[719277-26-6; 300801-52-9(mix E/Z); 1164521-02-1 (E)]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| TMS - Trans-2,3',4,5'-tetramethoxystilbene | Axon 2628
CAS [24144-92-1]
MF C18H20O4MW 300.35
Purity:
99%
Soluble in DMSO
Description
CYP1B1 inhibitor (IC50 values 6 nM, 300 nM, and 3100 nM for inhibition of CYP1B1, CYP1A1, and CYP1A2, resp.), that potentiates the inhibition of cell growth and induces apoptosis in human cancer cells. Moreover, TMS is a useful compound for characterizing the enzymatic properties of CYP1B1 and its contribution to hypertension and associated pathophysiology.
KEYWORDS: TMS | supplier | CYP1B1 inhibitor | Trans-2,3',4,5'-tetramethoxystilbene | tetramethoxystilbene | CAS [24144-92-1] | Cytochrome P450 | Aryl hydrocarbon hydroxylase | cell growth | apoptosis | cancer | hypertension | cardiovascular | | axonmedchem |
| RU 58841 | Axon 1680
CAS [154992-24-2]
MF C17H18F3N3O3MW 369.34
Purity:
99%
Soluble in DMSO
Description
A specific androgen receptor antagonist or anti-androgen; RU 58841 has a dramatic effect on hair regrowth.
This product is not intended/sold for (self-)diagnostic and/or therapeutic use.
References
Certificates
Categories
Extra info
N Obana et al. Inhibition of Hair Growth by Testosterone in the Presence of Dermal Papilla Cells from the Frontal Bald Scalp of the Postpubertal Stumptailed Macaque. Endocrinology 1997, 138(1), 356-361.
T Battmann et al. RU 58841, a new specific topical antiandrogen: A candidate of choice for the treatment of acne, androgenetic alopecia and hirsutism. J. Steroid Biochem. Mol. Biol. 1994, 48(1), 55-60.
HI Pan et al. Evaluation of RU58841 as an anti-androgen in prostate PC3 cells and a topical anti-alopecia agent in the bald scalp of stumptailed macaques. Endocrine 1998, 9(1) 39-43.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Endocrinology
Androgen (AR)
NR3C
Androgen receptor (AR) antagonist
Chemical name
4-(3-(4-hydroxybutyl)-4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile
Parent CAS No.
[154992-24-2]
Order
Size
Unit Price
Stock
5 mg
€80.00
In Stock | | axonmedchem |
| SPHINX31 | Axon 2714
CAS [1818389-84-2]
MF C27H24F3N5O2MW 507.51
Purity:
99%
Soluble in DMSO
Description
SPHINX31 is a highly potent, selective, and cell active SRPK1 inhibitor (IC50 value of 6 nM). Treatment with this inhibitor inhibited SRPK1 activity and phosphorylation of serine/arginine splicing factor 1 (SRSF1), resulting in alternative splicing of VEGF-A from pro-angiogenic to antiangiogenic isoforms. This property resulted in potent inhibition of blood vessel growth in models of choroidal angiogenesis in vivo.
KEYWORDS: SPHINX31 | supplier | SRPK1 inhibitor | SPHINX 31 | SPHINX-31 | CAS [1818389-84-2] | DNA-RNA | SRPK | Inhibitor | Enzymes | Neovascular Eye Disease | VEGF | SRSF1 | | axonmedchem |
| Voriconazole - Vfend | UK 109496 | Axon 2044
CAS [137234-62-9]
MF C16H14F3N5OMW 349.31
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Orally bioavailable CYP51 inhibitor; Antifungal agent; Voriconazole binds and inhibits ergosterol synthesis by inhibiting CYP450-dependent 14-α sterol demethylase (CYP51, P450-DM), resulting in a depletion of ergosterol in fungal cell membrane.
References
Certificates
Categories
Extra info
L.J. Scott et al. Voriconazole : a review of its use in the management of invasive fungal infections. Drugs. 2007, 67, 269-298.
M. Sandherr et al. Pharmacology and metabolism of voriconazole and Posaconazole in the treatment of invasive aspergillosis: review of the literature. Eur. J. Med. Res. 2011, 16, 139-144.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Immunology
EC 1.14.13.70
Cytochrome P450
Pfizer Licensed Products
Orally bioavailable CYP51 inhibitor; Antifungal agent
Chemical name
(2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[137234-62-9]
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Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| RD 162 | Axon 1532
CAS [915087-27-3]
MF C22H16F4N4O2SMW 476.45
Purity:
98%
Soluble in DMSO
Description
An orally active and very potent antagonist of androgen receptor (AR); Second-generation of antiandrogen for the treatment of advanced prostate cancer; highly recommended tool in AR research
References
Certificates
Categories
Extra info
C Tran et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science 2009, 324 (5928), 787-790.
C Harrison. Anticancer drugs: New approaches to anti-androgen activities. Nature Reviews Drug Discovery 2009, 8, 452-453.
CJ Hoimes and WK Kelley. Redefining hormone resistance in prostate cancer. Ther Adv Med Oncol. 2010, 2(2), 107–123.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Endocrinology
Androgen (AR)
NR3C
Androgen receptor (AR) antagonist
Chemical name
4-[7-(4-Cyano-3-trifluoromethyl-phenyl)-8-oxo-6-thioxo-5,7-diaza-spiro[3.4]oct-5-yl]-2-fluoro-N-methyl-benzamide
Parent CAS No.
[915087-27-3]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| Abiraterone - CB 7598 | Axon 1873
CAS [154229-19-3]
MF C24H31NOMW 349.51
Purity:
100%
Optical purity:
Optically pure
Moderately soluble in DMSO
Description
Inhibitor of the steroidal enzyme 17 α-hydroxylase/C17,20 lyase (CYP17A1); a drug used in castration-resistant prostate cancer (CRPC); active component of its formulated prodrug abiraterone acetate (Axon 1874), which is also available
References
Certificates
Categories
Extra info
G Attard et al. Selective blockade of androgenic steroid synthesis by novel lyase inhibitors as a therapeutic strategy for treating metastatic prostate cancer. BJU Int. 2005, 96 (9), 1241–1246.
JE Ang et al. CYP17 blockade by abiraterone: further evidence for frequent continued hormone-dependence in castration-resistant prostate cancer. Br. J. Cancer 2009, 100(5), 671–675.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Endocrinology
EC 1.14.99.9
Cytochrome P450
Inhibitor of CYP17A1
Chemical name
(3S,8R,9S,10R,13S,14S)-10,13-dimethyl-17-(pyridin-3-yl)-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol
Parent CAS No.
[154229-19-3]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| Abiraterone acetate - CB 7630 | JNJ 212082 | Axon 1874
CAS [154229-18-2]
MF C26H33NO2MW 391.55
Purity:
100%
Optical purity:
Optically pure
Poorly soluble in DMSO
Description
Orally administered prodrug of Abiraterone (Axon 1873); inhibitor of the steroidal enzyme 17 α-hydroxylase/C17,20 lyase (CYP17A1); a drug used in castration-resistant prostate cancer (CRPC)
References
Certificates
Categories
Extra info
G Attard et al. Selective blockade of androgenic steroid synthesis by novel lyase inhibitors as a therapeutic strategy for treating metastatic prostate cancer. BJU Int. 2005, 96 (9), 1241–1246.
JE Ang et al. CYP17 blockade by abiraterone: further evidence for frequent continued hormone-dependence in castration-resistant prostate cancer. Br. J. Cancer 2009, 100(5), 671–675.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Endocrinology
EC 1.14.99.9
Cytochrome P450
Prodrug of Abiraterone; Inhibitor of CYP17A1
Chemical name
(3S,8R,9S,10R,13S,14S)-10,13-dimethyl-17-(pyridin-3-yl)-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]phenanthren-3-yl acetate
Parent CAS No.
[154229-18-2]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| Tienilic Acid - Ticrynafan | Axon 1564
CAS [40180-04-9]
MF C13H8Cl2O4SMW 331.17
Purity:
99%
Soluble in DMSO
Description
Tienilic acid was found to act as a suicide substrate at the cytochrome P450 enzymes involved in drug metabolism. It is a good mechanism based inhibitor of CYP2C9 and seems to inactivate it stoichiometrically
References
Certificates
Categories
Extra info
JW Manier et al. Hepatotoxicity associated with ticrynafen – a uricosuric diuretic. Am. J. Gastroenterol. 1982, 77(6), 401–4.
P Jean et al. Oxidation of tienilic acid by human yeast-expressed cytochromes P450 2C8, 2C9, 2C18 and 2C19: Evidence that this drug is a mechanism-based inhibitor specific of cytochrome P450 2C9. Eur. J. Biochem. 1996, 241 797-804.
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
Miscellaneous
EC 1.14.13.80
Cytochrome P450
CYP2C10 Inhibitor
Chemical name
[2,3-Dichloro-4-(thiophene-2-carbonyl)-phenoxyl]-acetic acid
Parent CAS No.
[40180-04-9]
Order
Size
Unit Price
Stock
5 mg
€75.00
In Stock | | axonmedchem |
| PPP hydrochloride | Axon 1595
CAS [21602-56-2]
MF C14H21N.HClMW 239.78
Purity:
99%
Soluble in water
Description
Selective inactivator of human cytochrome P450 2B6 (CYP2B6)
References
Certificates
Categories
Extra info
RL Walsky and RS Obach. A Comparison of PPP, 1,1′,1″-Phosphinothioylidynetrisaziridine (ThioTEPA), Clopidogrel, and Ticlopidine as Selective Inactivators of Human Cytochrome P450 2B6. Drug Metab. Dsipos. (DMD). 2007, 35(11), 2053-2059.
J Chun et al. Mechanism-based inactivation of cytochromes P450 2B1 and P450 2B6 by 2-phenyl-2-(1-piperidinyl)propane. Drug Metab Dispos. 2000, 28(8), 905-911.
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
Miscellaneous
EC 1.14.14.1
Cytochrome P450
CYP2B6 inhibitor
Chemical name
1-(2-phenylpropan-2-yl)piperidine hydrochloride
Parent CAS No.
[92321-29-4]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Danoprevir - ITMN 191 | RG 7227 | R 7227 | Axon 1669
CAS [850876-88-9]
MF C35H46FN5O9SMW 731.83
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and orally active inhibitor of hepatitis C virus (HCV) NS3/4A serine protease (replicon IC50: 1.6 nM)
References
Certificates
Categories
Extra info
EJ Gane et al. Antiviral activity, safety, and pharmacokinetics of danoprevir / ritonavir plus PEG-IFN α-2a/RBV in hepatitis C patients. J Hepatol. 2011, 55(5), 972-979.
Certificate of Analysis
Material Safety Data Sheet
Immunology
Miscellaneous
HCV NS3 Serine Protease
HCV NS4A Serine Protease
EC 3.4.21.98
HCV NS3/4A serine protease inhibitor
Chemical name
(2R,6S,13aS,14aR,16aS,Z)-6-(tert-butoxycarbonylamino)-14a-(cyclopropylsulfonylcarbamoyl)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-2-yl 4-fluoroisoindoline-2-carboxylate
Parent CAS No.
[850876-88-9]
Order
Size
Unit Price
Stock
2 mg
€115.00
In Stock | | axonmedchem |
| Posaconazole - SCH 56592 | Noxafil | Axon 1557
CAS [171228-49-2]
MF C37H42F2N8O4MW 700.78
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
A triazole antifungal drug
References
Certificates
Categories
Extra info
JA Urbina et al. Antiproliferative Effects and Mechanism of Action of SCH 56592 against Trypanosoma (Schizotrypanum)cruzi: In Vitro and In Vivo Studies. Antimicrob. Agents Chemother. 1998, 42(7), 1771-1777.
DS Schiller and HB Fung. Posaconazole: an extended-spectrum triazole antifungal agent. Clin Ther 2007, 29(9), 1862–86.
EJ Rachwalski et al. Posaconazole: an oral triazole with an extended spectrum of activity. Ann Pharmacother 2008, 42 (10): 1429–38.
Certificate of Analysis
Material Safety Data Sheet
Immunology
Miscellaneous
EC 1.14.13.70
Cytochrome P450
Antifungal agent
Chemical name
4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-1-((2S,3S)-2-hydroxypentan-3-yl)-1H-1,2,4-triazol-5(4H)-one
Parent CAS No.
[171228-49-2]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| AG 7088 - Rupintrivir | Ruprintrivir | Axon 1571
CAS [223537-30-2]
MF C31H39FN4O7MW 598.66
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
An irreversible human rhinovirus (HRV) 3C protease inhibitor
References
Certificates
Categories
Extra info
G Witherell. AG-7088 Pfizer. Curr. Opin. Investig. Drugs. 2000, 1(3), 297-302.
AG-7088. Drugs Fut. 2000, 25, 1, 9
ST Worland et al. Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 3. Structure-activity studies of ketomethylene-containing peptidomimetics. J. Med. Chem. 1999, 42,(7), 1203.
SL Binford et al. In Vitro Resistance Study of Rupintrivir, a Novel Inhibitor of Human Rhinovirus 3C Protease. ANTIMICROB. AGENTS CHEMOTHER. 2007, 51(12), 4366–4373.
Certificate of Analysis
Material Safety Data Sheet
Immunology
HRV3C Protease
EC 3.4.22.28
HRV3C protease inhibitor
Chemical name
(E)-(S)-4-{(2R,5S)-2-(4-Fluoro-benzyl)-6-methyl-5-[(5-methyl-isoxazole-3-carbonyl)-amino]-4-oxo-heptanoylamino}-5-((S)-2-oxo-pyrrolidin-3-yl)-pent-2-enoic acid ethyl ester
Parent CAS No.
[223537-30-2]
Order
Size
Unit Price
Stock
1 mg
€95.00
In Stock | | axonmedchem |
| SB 265610 | Axon 1559
CAS [ 211096-49-0]
MF C14H9BrN6OMW 357.16
Purity:
99%
Soluble in DMSO
Description
Potent allosteric, inverse agonist/antagonist at the human chemokine CXCR2 receptor. SB-265610 antagonizes rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization, and rat neutrophil chemotaxis in a concentration-dependent manner (IC50 values 3.7 nM and 70 nM, respectively).
KEYWORDS: SB 265610 | supplier | CXCR2 antagonist | SB265610 | CAS [ 211096-49-0] | Chemokine | Inverse agonist | Antagonist | C-X-C | neutrophil | chemotaxis | calcium mobilization | GPCR | | axonmedchem |
| Nelfinavir mesylate - AG 1343 | Axon 1553
CAS [159989-65-8]
MF C32H45N3O4S.CH4O3SMW 663.89
Purity:
99%
Soluble in DMSO
Description
Orally active HIV protease inhibitor, with KI values to be 2nM (HIV-1)
References
Certificates
Categories
Extra info
P Pyrko. HIV-1 protease inhibitors nelfinavir and atazanavir induce malignant glioma death by triggering endoplasmic reticulum stress. Cancer Res. 2007, 67, 10920–8.
JJ Gills et al. Nelfinavir, A Lead HIV Protease Inhibitor, Is a Broad-Spectrum, Anticancer Agent that Induces Endoplasmic Reticulum Stress, Autophagy, and Apoptosis In vitro and In vivo. Clin. Cancer Res. 2007, 13(17), 5183–5194.
WA Chow et al. Anti-HIV drugs for cancer therapeutics: back to the future?. Lancet Oncol. 2009, 10 (1), 61–71.
Certificate of Analysis
Material Safety Data Sheet
Immunology
HIV-1 Protease
EC 3.4.23.16
Pfizer Licensed Products
HIV-1 protease inhibitor
Chemical name
(3S,4aS,8aS)-N-tert-butyl-2-((2R,3R)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)-4-(phenylthio)butyl)decahydroisoquinoline-3-carboxamide methanesulfonate
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[159989-64-7]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| Dapivirine - R 147681 | TMC 120 | Axon 1534
CAS [244767-67-7]
MF C20H19N5MW 329.40
Purity:
99%
Soluble in DMSO
Description
Potent non-nucleoside reverse transcriptase inhibitor (NNRTI); an antiretroviral compound designed to prevent or interrupt HIV replication in human cells; safe and tolerable as potential vaginal microbicide
References
Certificates
Categories
Extra info
A David Woolfson et al. Intravaginal ring delivery of the reverse transcriptase inhibitor TMC 120 as an HIV microbicide. Int. J. Pharmaceutics. 2006, 325(1-2), 82-89.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
RT
p53-Tumor Suppression
DNA-damage Response
EC 2.7.7.49
NNRT inhibitor
Chemical name
4-[4-(2,4,6-Trimethyl-phenylamino)-pyrimidin-2-ylamino]-benzonitrile
Parent CAS No.
[244767-67-7]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| BMS 232632 - Atazanavir | CGP 73547 | Axon 1441
CAS [198904-31-3]
MF C38H52N6O7MW 704.86
Purity:
99%
Soluble in DMSO
Description
Orally active protease inhibitor (PI); antiretrovirals used to treat infection of human immunodeficiency virus (HIV)
References
Certificates
Categories
Extra info
P Pyrko. HIV-1 protease inhibitors nelfinavir and atazanavir induce malignant glioma death by triggering endoplasmic reticulum stress. Cancer Research 2007, 67, 10920–8.
T Ly & M Ruiz. Prolonged QT interval and torsades de pointes associated with atazanavir therapy Question: Have patients developed Liver stones as a side-effect of this medication?". Clin Infect Dis 2007, 44 (6), e67–8.
Certificate of Analysis
Material Safety Data Sheet
Immunology
Non Selective
EC 3.4.23.16
Protease inhibitor
Chemical name
3,12-bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-, dimethyl ester, [3S-(3R*,8R*,9R*,12R*)]-
Parent CAS No.
[198904-31-3]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| A1B1 hydrochloride | Axon 1179
CAS [N.A.]
MF C23H25ClFN3O2.HClMW 466.38
Purity:
99%
Optical purity:
>98% ee
Soluble in DMSO
Description
Potent and orally active chemokine CCR1 antagonist
References
Certificates
Categories
Extra info
L Revesz et al. Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis. Bioorg. Med. Chem. Lett. 2005, 15(23), 5160-5164.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
Pain & Inflammation
A1
Chemokine
CCR1 antagonist
Chemical name
N-(5-Chloro-2-{(E)-3-[(R)-4-(4-fluoro-benzyl)-2-methyl-piperazin-1-yl]-3-oxo-propenyl}-phenyl)-acetamide Hydrochloride
Parent CAS No.
[685534-25-2]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| MG 149 | Axon 1785
CAS [1243583-85-8]
MF C22H28O3MW 340.46
Purity:
99%
Soluble in DMSO
Description
A novel anacardic acid analog; potent and selective inhibitor of the MYST family (Tip60 and MOZ) of histone acetyltransferase (HAT). In addition, it effectively inhibits acetyltransferase activity of HeLa cells nuclear extracts.*Sold in collaboration with RuG (University of Groningen)
KEYWORDS: MG 149 | supplier | Tip60 HAT inhibitor | MG149 | MG-149 | CAS [1243583-85-8] | Histone | MYST family | MOZ | acetyltransferase | anacardic acid | inflammation | | axonmedchem |
| C 646 | Axon 1781
CAS [328968-36-1]
MF C24H19N3O6MW 445.42
Purity:
99%
Moderately soluble in DMSO
Description
Competitive p300/CBP histone acetyltransferase (HAT) inhibitor with a Ki of 400 nM; Selective versus other acetyltransferases
References
Certificates
Categories
Extra info
EM Bowers et al. Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. Chem. Biol. 2010, 17, 471-482. [onlne]
NY Crump et al. Dynamic acetylation of all lysine-4 trimethylated histone H3 is evolutionarily conserved and mediated by p300/CBP. Proc Natl Acad Sci U S A. 2011, 108(19), 7814-7819.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
HAT
EC 2.3.1.48
HAT inhibitor (p300/CBP selective)
Chemical name
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Parent CAS No.
[328968-36-1]
Order
Size
Unit Price
Stock
2 mg
€60.00
In Stock | | axonmedchem |
| Anacardic acid A - Pentadecylsalicylic acid, 6- | Axon 1490
CAS [16611-84-0]
MF C22H36O3MW 348.52
Purity:
98%
Soluble in DMSO
Description
A cell-permeaable, non-competitive inhibitor of histone acetyl transferase (HAT)
References
Certificates
Categories
Extra info
K. Balasubramanyam et al. Small molecule modulators of histone acetyltransferase p300. J. Biol. Chem. 2003, 278, 19134.
Y. Sun et al. Inhibition of histone acetyltransferase activity by anacardic acid sensitizes tumor cells to ionizing radiation. FEBS Lett. 2006, 580, 4353.
B Sung et al. Anacardic acid, an inhibitor of histone acetyltransferase, suppresses expression of NF-kappaB-regulated gene products involved in cell survival, proliferation, invasion, and inflammation. Blood. 2008, 111(10), 4880-91.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
HAT
EC 2.3.1.48
HAT inhibitor
Chemical name
2-Hydroxy-6-pentadecyl-benzoic acid
Parent CAS No.
[16611-84-0]
Order
Size
Unit Price
Stock
10 mg
€60.00
In Stock | | axonmedchem |
| BAY 57-1293 - Pritelivir | AIC 316 | Axon 2266
CAS [348086-71-5]
MF C18H18N4O3S2MW 402.49
Purity:
99%
Soluble in DMSO
Description
Potent helicase-primase inhibitor (HPI) effective against herpes simplex virus (HSV) infections with IC50 value of 20 nM for inhibition of the replication of both HSV-1 and HSV-2 in Vero cells, and ED50 value of 0.5 mg/kg for both HSV-1 and HSV-2 in the murine lethal challenge model of disseminated herpes. BAY 57-1293 in vivo was found to be superior compared to all compounds currently used to treat HSV infections, and is active also against acyclovir-resistant mutant strains which carry mutations in the tk or DNA pol genes.
References
Certificates
Categories
Extra info
J.J. Crute et al. Herpes simplex virus helicase-primase inhibitors are active in animal models of human disease. Nat. Med. 2002, 8, 386-391.
U.A. Betz et al. Potent in vivo antiviral activity of the herpes simplex virus primase-helicase inhibitor BAY 57-1293. Antimicrob. Agents Chemother. 2002, 46, 1766-1772.
S. Biswas et al. The helicase primase inhibitor, BAY 57-1293 shows potent therapeutic antiviral activity superior to famciclovir in BALB/c mice infected with herpes simplex virus type 1. Antiviral Res. 2007, 75, 30-35.
Certificate of Analysis
Material Safety Data Sheet
Immunology
Helicase-Primase
EC 3.6.4.12
Potent helicase-primase inhibitor, effective against herpes simplex virus (HSV) infections
Chemical name
N-Methyl-N-(4-methyl-5-sulfamoylthiazol-2-yl)-2-(4-(pyridin-2-yl)phenyl)acetamide
Parent CAS No.
[348086-71-5]
Order
Size
Unit Price
Stock
5 mg
€80.00
In Stock | | axonmedchem |
| FIPI hydrochloride | Axon 2281
CAS [N.A.]
MF C23H24FN5O2.HClMW 457.93
Purity:
99%
Soluble in DMSO
Description
Phospholipase D (PLD) inhibitor (IC50 values of 20-25 nM for both PLD1 and PLD2) that rapidly blocks in vivo phosphatidic acid (PA) production with subnanomolar potency.
FIPI does inhibit PLD regulation of F-actin cytoskeleton reorganization, PIP2 availability, cell spreading, and chemotaxis, indicating potential utility for it as a therapeutic for autoimmunity and cancer metastasis.
References
Certificates
Categories
Extra info
W. Su et al. 5-Fluoro-2-indolyl des-chlorohalopemide (FIPI), a phospholipase D pharmacological inhibitor that alters cell spreading and inhibits chemotaxis. Mol. Pharmacol. 2009, 75, 437-446.
L. Monovich et al. Optimization of halopemide for phospholipase D2 inhibition. Bioorg. Med. Chem. Lett. 2007, 17, 2310-2311.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Pain & Inflammation
EC 3.1.4.4
PLD
Phospholipase D (PLD) inhibitor that blocks phosphatidic acid (PA) production in vivo
Chemical name
5-fluoro-N-(2-(4-(2-oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)piperidin-1-yl)ethyl)-1H-indole-2-carboxamide hydrochloride
Parent CAS No.
[939055-18-2]
Order
Size
Unit Price
Stock
5 mg
€100.00
In Stock | | axonmedchem |
| NSC 23005 sodium | Axon 2695
CAS [1796596-46-7]
MF C13H16NNaO4SMW 305.33
Purity:
100%
Soluble in water and DMSO
Description
Novel small molecule inhibitor of INK4C (p18(INK4C) or p18) that promotes expansion of both murine and human HSCs (ED50 value 5.21 nM). This p18SMI shows no significant cytotoxicity toward 32D cells or HSCs, nor does it augment leukemia cell proliferation.
KEYWORDS: NSC 23005 sodium | supplier | p18-INK4C inhibitor | NSC23005 sodium | NSC-23005 sodium | CAS [1796596-46-7] | [6314-70-1] | Cyclin Dependent Kinase | INK4 | CDK4 | CDK6 | Regulator Protein | cell cycle | apoptosis | expansion | HSC | Hematopoietic | stem cell | mitotic | | axonmedchem |
| GSK-LSD1 | Axon 2375
CAS [N.A.]
MF C14H20N2.2HClMW 289.24
Purity:
99%
Optical purity:
mixture of trans-diastereomers
Soluble in water and DMSO
Description
Irreversible inhibitor of the KDM1 family histone demethylase LSD1 (IC50 value 16 nM). GSK-LSD1 is >1000 fold selective over closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B), induces gene expression changes in cancer cell lines (average EC50 <5 nM), and inhibits cancer cell line growth (average EC50 <5 nM).
References
Certificates
Categories
Extra info
O. Munoz et al. Aryl- and heteroarylcyclopropylamine compounds as LSD1 inhibitors and their preparation. PCT Int. Appl. (2013), WO 2013057320 A1 20130425.
D.P. Mould et al. Reversible Inhibitors of LSD1 as Therapeutic Agents in Acute Myeloid Leukemia: Clinical Significance and Progress to Date. Med Res Rev. 2014 Nov 24.
J. McGrath et al. Targeting histone lysine methylation in cancer. Pharmacol Ther. 2015 Jan 9. pii: S0163-7258(15)00003-0.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
Immunology
EC 1.14.11
Histone demethylase
Irreversible inhibitor of the KDM1 family histone demethylase LSD1
Chemical name
rel-N-((1R,2S)-2-phenylcyclopropyl)piperidin-4-amine dihydrochloride
Parent CAS No.
[1431368-48-7]
Order
Size
Unit Price
Stock
10 mg
€110.00
In Stock | | axonmedchem |
| iMDK | Axon 2258
CAS [881970-80-5]
MF C21H13FN2O2SMW 376.40
Purity:
99%
Soluble in DMSO
Description
MDK expression inhibitor; iMDK inhibits specifically and dose-dependently the expression of Midkine (MDK) in H441 lung adenocarcinoma cells, but does not inhibit PTN (Pleiotrophin), which has considerable homology to MDK. iMDK induces apoptotosis in MDK-expressing H441 lung adenocarcinoma cells by suppression of the PI3K/Akt pathway but not the MAPK pathway. iMDK does not inhibit another growth factor VEGF.
KEYWORDS: iMDK | Midkine expression inhibitor | CAS [881970-80-5] | NF-κB Pathway | Midkine | Inhibitor | Proteins | cytokine | NF-êB | PI3K | Akt | Apoptosis | Carcinoma | Lung cancer | | axonmedchem |
| ASB14780 | Axon 2578
CAS [1069046-00-9]
MF C31H27NO3.C4H11NO3MW 582.69
Purity:
99%
Soluble in DMSO
Description
Potent, orally available inhibitor of cytosolic phospholipase A2α (cPLA2α, a group IVA phospholipase A2, aka IVA-PLA2) with an IC50 value 0.020 µM in vitro and 0.54 - 0.64 µM in whole blood assay (guinea pig and human, respectively)) with anti-inflammatory efficacy in ear edema and asthma models, and potentially useful for the treatment of nonalcoholic fatty liver diseases, including fatty liver and hepatic fibrosis. ASB14780 markedly attenuated expression of smooth muscle a-actin (a-SMA) protein and the mRNA expression of collagen 1a2, a-SMA, and TGFb1 in the liver, and inhibited the expression of monocyte/macrophage markers. Sold as tromethamine (THAM) salt, as it was used in original publication.
KEYWORDS: ASB14780 | supplier | cPLA2α inhibitor | ASB-14780 | CAS [1069046-00-9] | [1069044-40-1] | Phospholipids | cPLA2 | phospholipase | anti-inflammatory | edema | asthma | pulmonary diseases | fatty liver diseases | hepatic fibrosis | actin | collagen | TGFb1 | | axonmedchem |
| HAMNO - NSC 111847 | Axon 2390
CAS [138736-73-9]
MF C17H13NO2MW 263.29
Purity:
99%
Soluble in DMSO
Description
Novel protein interaction inhibitor of replication protein A (RPA), a protein involved in the ATR/Chk1 pathway. HAMNO selectively binds the N-terminal DBD-F domain of RPA70, effectively inhibiting critical RPA protein interactions that rely on this domain. HAMNO inhibits both ATR autophosphorylation and phosphorylation of RPA32 Ser33 by ATR. Candidate therapeutic for cancer treatment, as it enhances the constitutive and oncogene-induced replication stress in cancer cells.
References
Certificates
Categories
Extra info
J.G. Glanzer et al. RPA inhibition increases replication stress and suppresses tumor growth. Cancer Res. 2014 Sep 15;74(18):5165-72.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
DNA-damage Response
RPA
Novel protein interaction inhibitor of replication protein A (RPA)
Chemical name
(Z)-1-((2-hydroxyphenylamino)methylene)naphthalen-2(1H)-one
Parent CAS No.
[138736-73-9]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| SP 2509 | Axon 2864
CAS [1423715-09-6]
MF C19H20ClN3O5SMW 437.90
Purity:
98%
Soluble in DMSO
Description
SP 2509 is a potent, reversible, and specific LSD1 inhibitor with an IC50 value of 0.013 µM (Ki value of 31 nM). Moreover, SP 2509 inhibits proliferation and survival in several cancer cell lines, including breast and colorectal cancer.
KEYWORDS: SP 2509 | supplier | LSD1 inhibitor | SP2509 | SP-2509 | CAS [1423715-09-6] | CAS [1287421-04-8] | Histone | Histone demethylase | Inhibitor | Enzymes | BHC 110 inhibitor VII | Histone Lysine Demethylase Inhibitor XIV | KIAA 1718 inhibitor VII | LSD 1 inhibitor VII | | axonmedchem |
| KDM5 inhibitor compound 48 | Axon 2809
CAS [1628210-26-3]
MF C17H20N6OMW 324.38
Purity:
99%
Soluble in DMSO
Description
Potent, selective and orally bioavailable KDM5 inhibitor (IC50 value of 15.1 nM for KDM5A) with improved cell potency (EC50 value of 0.34 μM, H3K4Me3 level in PC9 cells). Chemical probe suitable for studying KDM5 biological functions in vivo.
KEYWORDS: KDM5 inhibitor compound 48 | supplier | KDM5 inhibitor | CAS [1628210-26-3] | Histone demethylase | Inhibitor | Enzymes | Orally bioavailable | PC9 | | axonmedchem |
| AZD2716 | Axon 2661
CAS [1845753-81-2]
MF C24H23NO3MW 373.44
Purity:
99%
Optical purity:
98% e.e.
Soluble in 0.1N NaOH (aq) and DMSO
Description
AZD2716 is a novel, potent sPLA2 inhibitor (IC50 values of 10, 40, and 400 nM for sPLA2-IIa, -V, and -X, respectively) with excellent preclinical pharmacokinetic properties across species, clear in vivo efficacy, and minimized safety risk. When incubated with HepG2 cells, AZD2716 effectively inhibited sPLA2 activity (IC50 value of <14 nM) and suppressed production of sPLA2-IIa (IC50 value of 176 nM). AZD2716 also demonstrated significant sPLA2 activity inhibition (IC50 value of 56 nM) in atherosclerotic plaque homogenates. | | axonmedchem |
| AZ 20 | Axon 2345
CAS [1233339-22-4]
MF C21H24N4O3SMW 412.51
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent, orally active and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity (IC50 value 5 nM). AZ 20 potently inhibits the growth of LoVo colorectal adenocarcinoma tumor cells in vitro, and is a useful compound to explore ATR pharmacology in vivo.
KEYWORDS: AZ 20 | supplier | ATR inhibitor | AZ20 | AZ-20 | CAS [1233339-22-4] | DNA-damage response | ATR | ATM | DNA | damage control | cancer | oncology | Checkpoint | cell cycle control | | axonmedchem |