| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| Levofloxacin Q-acid | Axon 2242
CAS [100986-89-8]
MF C13H9F2NO4MW 281.21
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N NaOH(aq) and DMSO
Description
Inhibitor of bacterial DNA gyrase and topoisomerase IV with a minimum inhibitory concentration (MIC) of 0.75 μg/mL against penicillin-resistant Streptococcus pneumoniae.
Analogue of Trovafloxacin (Axon 2100).
References
Certificates
Categories
Extra info
B. Guruswamy et al. Synthesis, Characterization, Antimicrobial Activity of Novel N-Substituted ß-Hydroxy Amines and ß-Hydroxy Ethers Contained Chiral Benzoxazine Fluoroquinolones. Lett. Drug Design & Discov. 2013, 10, 86-93.
E. Hershberger et al. Activities of trovafloxacin, gatifloxacin, clinafloxacin, sparfloxacin, levofloxacin, and ciprofloxacin against penicillin-resistant Streptococcus pneumoniae in an (...). Antimicrob. Agents Chemother. 2000, 44, 598-601.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Immunology
DNA-damage Response
EC 5.99.1.3
TOPO
Antibiotics
Inhibitor of bacterial DNA gyrase and topoisomerase IV
Chemical name
(S)-9,10-difluoro-3-methyl-7-oxo-3,7-dihydro-2H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid
Parent CAS No.
[100986-89-8]
Order
Size
Unit Price
Stock
50 mg
€55.00
In Stock | | axonmedchem |
| CPI 4203 | Axon 2622
CAS [1628214-07-2]
MF C16H14N4OMW 278.31
Purity:
99%
Soluble in DMSO
Description
Selective inhibitor of KDM5 demethylases, structurally related to CPI 455 (Axon 2573) but ~25-fold less potent (IC50 value 250 nM for inhibition of full length KDM5A). Control compound to be used in combination with CPI 455 (Axon 2573).
KEYWORDS: CPI 4203 | supplier | KDM5 inhibitor | CPI4203 | CAS [1628214-07-2] | Histone demethylase | Inhibitor | H3K4 | KDM5A | lysine | methylation | drug tolerance | cancer | DTP | SET-domain | negative control | CPI455 | | axonmedchem |
| CPI 455 | Axon 2573
CAS [1628208-23-0]
MF C16H14N4OMW 278.31
Purity:
99%
Soluble in DMSO
Description
Selective inhibitor of KDM5 demethylases (IC50 value 10 nM for inhibition of full length KDM5A) that specifically alters H3K4 methylation in several cell contexts and reduces survival of drug-tolerant cancer cells. CPI-455 possesses the target specificity required for an in vitro tool compound for exploring KDM5-dependent disease biology, including drug tolerance.
Note: CPI 455 can be used in combination with a less potent control compound, by the authors of the 2016 Nature publication referred to as CPI 4203 (Axon 2622).
KEYWORDS: CPI 455 | supplier | KDM5 inhibitor | CPI455 | CAS [1628208-23-0] | Histone demethylase | Inhibitor | H3K4 | KDM5A | lysine | methylation | drug tolerance | cancer | DTP | SET-domain | | axonmedchem |
| TAS-103 dihydrochloride - BMS 247615 dihydrochloride | Axon 2914
CAS [174634-09-4]
MF C20H19N3O2.2HClMW 406.31
Purity:
99%
Soluble in water and DMSO
Description
TAS-103 dihydrochloride is an anticancer agent targeting topoisomerases I and II with IC50 values of 2 µM and 6.5 µM, respectively. Moreover, TAS-103 dihydrochloride has a strong cytotoxic effect on P388 and KB cells with IC50 values of 0.0011 µM and 0.0096 µM, respectively. Also, TAS-103 has strong inhibitory effects on the growth of various mouse and human solid tumors in vivo, as well as high antitumor activity against lung metastatic cancer.
KEYWORDS: TAS-103 dihydrochloride | supplier | Topo 1/2 inhibitor | BMS 247615 dihydrochloride | TAS-103 | TAS103 | BMS247615 | BMS-247615 | CAS [174634-08-3] | CAS [174634-09-4] | DNA-RNA | TOPO | Inhibitor | Enzymes | Topoisomerase | Lung cancer | | axonmedchem |
| BAY 1895344 | Axon 2918
CAS [1876467-74-1 ]
MF C20H21N7OMW 375.43
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
BAY 1895344 is a potent, highly selective and orally available ATR inhibitor (IC50 value of 7 nM), which potently inhibits proliferation of a broad spectrum of human tumor cell lines (median IC50 value of 78 nM). BAY 1895344 exhibits strong in vivo anti-tumor efficacy in monotherapy in a variety of xenograft models of different indications that are characterized by DDR deficiencies, inducing stable disease in ovarian and colorectal cancer or even complete tumor remission in mantle cell lymphoma models.
KEYWORDS: BAY 1895344 | supplier | ATR inhibitor | BAY1895344 | BAY-1895344 | CAS [1876467-74-1] | DNA-damage response | ATR | Inhibitor | Enzymes | Ovarian | Colorectal | Mantle cell lymphoma | | axonmedchem |
| Solithromycin - CEM 101 | OP 1068 | Axon 2606
CAS [760981-83-7]
MF C43H65FN6O10MW 845.01
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Fluoroketolide antibiotic with reported high potency against diverse groups of Gram-positive and Gram-negative bacteria (MIC50 values 0.015 μg/mL and 4 μg/mL, respectively). Solithromycin (CEM-101 or OP-1068) binds to multiple sites of the bacterial large ribosomal subunit (23S rRNA) near the ribosomal exit tunnel.
KEYWORDS: Solithromycin | supplier | Antibiotic | CEM 101 | OP 1068 | CEM101 | OP1068 | CAS [760981-83-7] | DNA-RNA | Peptidyl Transferase | Inhibitor | ribosome | 23S | fluoro-ketolide | gram-positive | gram-negative | bacteria | E.Coli | Staphylococcus aureus | | axonmedchem |
| KKL-10 | Axon 2802
CAS [952849-76-2]
MF C14H10BrN3O2SMW 364.22
Purity:
99%
Soluble in DMSO
Description
KKL-10 is a ribosome rescue (trans-translation) inhibitor which exhibited exceptional antimicrobial activity against both attenuated (MIC value of 0.12 µg/ml) and fully virulent strains of Francisella tularensis (MIC value of 0.48 µg/ml) in vitro and during ex vivo infection.
KEYWORDS: KKL-10 | supplier | Ribosome rescue inhibitor | KKL10 | KKL 10 | CAS [952849-76-2] | Ribosomes | trans-translation | Inhibitor | | axonmedchem |
| CS1 | Axon 2391
CAS [1448009-94-6]
MF C16H12O3MW 252.26
Purity:
99%
Soluble in DMSO
Description
TOPO IIα inhibitor with broad-spectrum in vitro antitumor effects (IC50 values 4.3 µM, 11.5 µM, and 4.6 µM for inhibition of proliferation of breast cancer MDA-MB-231, human lung cancer A549 and human cervical cancer HeLa cell lines, respectively). CS1 functions as a Topo II poison to stabilize Topo II/DNA complex, which leads to DNA damage, cell cycle arrest at G2/M phase and apoptosis, and is 6–10-fold less cytotoxic against HL7702 and HUVEC cells compared with etoposide.
References
Certificates
Categories
Extra info
W. Chen et al. Design and synthesis of 2-phenylnaphthalenoids as inhibitors of DNA topoisomeraseIIα and antitumor agents. Eur J Med Chem. 2014 Oct 30;86:782-96.
Y. Shen et al. CS1 is a novel topoisomerase IIα inhibitor with favorable drug resistance profiles. Biochem Biophys Res Commun. 2014 Oct 24;453(3):302-8.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Immunology
DNA-damage Response
EC 5.99.1.3
TOPO
TOPO IIα inhibitor with broad-spectrum in vitro antitumor effects
Chemical name
4-(6-hydroxynaphthalen-2-yl)benzene-1,2-diol
Parent CAS No.
[1448009-94-6]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| Clindamycin - Dalacine | U 21251 | Axon 2063
CAS [18323-44-9]
MF C18H33ClN2O5SMW 424.98
Purity:
100%
Soluble in DMSO
Description
A bacterial protein synthesis inhibitor; a Lincosamide antibiotic; stops the growth of bacteria by disrupting their production of proteins; inhibits the ribosomal peptidyltransferase
References
Certificates
Categories
Extra info
JG Bartlett et al. Clindamycin-associated colitis due to a toxin-producing species of Clostridium in hamsters. J. Infect. Diseases 1977, 136(5), 701-705.
J Sutcliffe, A Tait-Kamradt, and L Wondrack. Streptococcus pneumoniae and Streptococcus pyogenes resistant to macrolides but sensitive to clindamycin: a common resistance pattern (...). Antimicrob. Agents Chemother. 1996, 40(8), 1817-1824.
Certificate of Analysis
Material Safety Data Sheet
Immunology
EC 2.3.2.12
Peptidyl Transferase
Pfizer Licensed Products
Antibiotics
Inhibitor of peptidyl transferase; Antibiotic
Chemical name
(2S,4R)-N-((1S,2S)-2-chloro-1-((2R,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2H-pyran-2-yl)propyl)-1-methyl-4-propylpyrrolidine-2-carboxamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[18323-44-9]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| PF 05081090 - PF 5081090 | Axon 2113
CAS [1312473-63-4]
MF C18H21FN2O6SMW 412.43
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Very potent antibacterial LpxC inhibitor for the treatment of serious gram-negative infections (Pseudomonas aeruginosa (Pae) enzyme potency (Pae IC50) of 1.1 nM)
References
Certificates
Categories
Extra info
JI Montgomery et al. Pyridone methylsulfone hydroxamate LpxC inhibitors for the treatment of serious gram-negative infections. J. Med. Chem. 2012, 55(4), 1662-1670.
MF Brown et al. Potent Inhibitors of LpxC for the Treatment of Gram-Negative Infections. J. Med. Chem. 2012, 55(2), 914–923.
Certificate of Analysis
Material Safety Data Sheet
Immunology
LpxC
EC 3.5.1.108
Pfizer Licensed Products
Antibiotics
LpxC inhibitor for treatment of gram-negative infections
Chemical name
(R)-4-(4-(2-fluoro-4-methoxyphenyl)-2-oxopyridin-1(2H)-yl)-N-hydroxy-2-methyl-2-(methylsulfonyl)butanamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[1312473-63-4]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| Linezolid - Zyvox | PNU 100766 | U 100766 | Axon 2048
CAS [165800-03-3]
MF C16H20FN3O4MW 337.35
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Protein synthesis inhibitor; antibiotic; stops the growth of bacteria by disrupting their production of proteins; inhibits the ribosomal peptidyltransferase; antibacterial agent for the treatment of multidrug-resistant gram-positive bacterial infections
References
Certificates
Categories
Extra info
SJ Brickner et al. Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections. J. Med. Chem. 2008, 51(7), 1981-1990.
MR Barbachyn, CW Ford. Oxazolidinone structure-activity relationships leading to linezolid. Angew. Chem. Int. Ed. Engl. 2003, 42(18), 2010-23.
SJ Brickner et al. Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections. J. Med. Chem. 1996, 39(3), 673-9.
U Patel et al. Oxazolidinones mechanism of action: inhibition of the first peptide bond formation. J. Biol. Chem. 2001, 276(40), 37199-205.
CE Barry and JS Blanchard. The Chemical Biology of New Drugs in Development for Tuberculosis. Curr. Opin. Chem. Biol. 2010, 14(4), 456–466.
Certificate of Analysis
Material Safety Data Sheet
Immunology
EC 2.3.2.12
Peptidyl Transferase
Pfizer Licensed Products
Antibiotics
Protein synthesis inhibitor; antibiotic
Chemical name
(S)-N-((3-(3-fluoro-4-morpholinophenyl)-2-oxooxazolidin-5-yl)methyl)acetamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[165800-03-3]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| Sulbactam sodium - CP 45899 sodium | Axon 2041
CAS [69388-84-7]
MF C8H10NNaO5SMW 255.22
Purity:
98%
Soluble in water and DMSO
Description
An irreversible inhibitor of β-lactamase; it binds the enzyme and does not allow it to interact with the antibiotic
References
Certificates
Categories
Extra info
C Urban et al. Effect of Sulbactam on Infections Caused by Imipenem-Resistant Acinetobacter calcoaceticus Biotype anitratus. J. Infect. Dis. 1993, 167(2), 448-451.
JK Noguchi, MA Gill. Sulbactam: a beta-lactamase inhibitor. Clin. Pharm. 1988, 7(1), 37-51.
Certificate of Analysis
Material Safety Data Sheet
Immunology
β-Lactamase (Serine)
EC 3.5.2.6
Pfizer Licensed Products
Antibiotics
An irreversible inhibitor of β-lactamase
Chemical name
(2S,5R)-4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, 3,3-dimethyl-7-oxo-, 4,4-dioxide sodium salt
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[68373-14-8]
Order
Size
Unit Price
Stock
25 mg
€70.00
In Stock | | axonmedchem |
| BMS 303141 | Axon 2506
CAS [943962-47-8]
MF C19H15Cl2NO4SMW 424.30
Purity:
100%
Soluble in DMSO and Ethanol
Description
Cell-permeable ATP-citrate lyase (ACL) inhibitor (IC50 value 0.13 µM in vitro, and 8 µM for inhibition of total lipid syntheses in HepG2 cells). When administered to mice fed on a high-fat diet, it produced an approximate 20–30% lowering in plasma cholesterol and triglycerides, as well as a 30–50% decrease in fasting plasma glucose, as well as an inhibition of weight gain. BMS 303141 also showed inhibitory effects for other metabolic disease related targets such as ACC1 and ACC2 (IC50 values 6 µM and 12 µM, respectively).
KEYWORDS: BMS 303141 | supplier | ACL inhibitor | BMS303141 | CAS [943962-47-8] | ADP | ACL | ATP-citrate lyase | Inhibitor | metabolic disorders | diabetes | obesity | dyslipidemia | acetyl-CoA | fatty acid | cholesterol | cardiovascular | LDL | HDL | weight gain | triglycerides | | axonmedchem |
| RTA 408 - Omaveloxolone | Axon 2497
CAS [1474034-05-3]
MF C33H44F2N2O3MW 554.71
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Synthetic triterpenoid that potently activates the antioxidative transcription factor Nrf2 (nuclear factor erythroid 2-related factor 2) and inhibits the proinflammatory transcription factor NF-κB at low concentrations. RTA 408 dose-dependently reduced NO concentrations (IC50 value 4.4 Nm). At higher concentrations, RTA 408 inhibited tumor cell growth (GI50 value 260 nM) and increased caspase activity in tumor cell lines and is a highly effective mitigator of steady state hematopoiesis.
KEYWORDS: RTA 408 | NRF2 acitivator | Axon 2497 | Omaveloxolone | RTA408 | CAS [1474034-05-3] | DNA-RNA | NRF | Activator | Transcription Factor | NF-E2L2 | ROS | NO | nuclear factor erythroid 2-related factor 2 | JNK | NF-κB | inflammatory | radiation | mitigator | hematopoiesis | | axonmedchem |
| LpxC inhibitor 1a | Axon 1939
CAS [1289620-49-0]
MF C18H21NO4SMW 347.43
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Potent antibacterial LpxC inhibitor (IC50: 1.37 nm) for the treatment of gram-negative infections
References
Certificates
Categories
Extra info
MF Brown et al. Potent Inhibitors of LpxC for the Treatment of Gram-Negative Infections. J. Med. Chem. 2012, 55 (2), 914–923.
Certificate of Analysis
Material Safety Data Sheet
Immunology
LpxC
EC 3.5.1.108
Antibiotics
Potent antibacterial LpxC inhibitor (gram-negative infections)
Chemical name
(R)-4-(biphenyl-4-yl)-N-hydroxy-2-methyl-2-(methylsulfonyl)butanamide
Parent CAS No.
[1289620-49-0]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| CHIR 090 | Axon 2000
CAS [728865-23-4]
MF C24H27N3O5MW 437.49
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
Very potent and selective UDP-3-O-(R-3-hydroxyacyl)-N-acetylglucosamine deacetylase LpxC inhibitor (Ki: 1-2 nM and slow, tight-binding)
KEYWORDS: CHIR 090 | supplier | LpxC inhibitor | CHIR090 | CHIR-090 | CAS [728865-23-4] | Lipid A precursor | LpxC | Inhibitor | UDP | glucosamine | | axonmedchem |
| ML385 | Axon 2671
CAS [846557-71-9]
MF C29H25N3O4SMW 511.59
Purity:
99%
Soluble in DMSO
Description
ML385 is an inhibitor of nuclear factor erythroid 2-related factor 2 (NRF2) (IC50 value 1.9 μM), blocks NRF2 transcriptional activity, and enhances the efficacy of carboplatin and other chemotherapeutic drugs in lung cancer cells (NSCLC). Specifically, ML385 binds to Neh1, the Cap ‘N’ Collar Basic Leucine Zipper (CNC-bZIP) domain of NRF2, and interferes with the binding of the V-Maf Avian Musculoaponeurotic Fibrosarcoma Oncogene Homologue G (MAFG)-NRF2 protein complex to regulatory DNA binding sequences. ML385 shows specificity and selectivity for NSCLC cells with KEAP1 mutation.
KEYWORDS: ML385 | supplier | NRF2 inhibitor | ML-385 | ML 385 | CAS [846557-71-9] | DNA-RNA | NRF | Keap | Inhibitor | Transcription Factors | NSCLC | KEAP1 | NRF2 | CNC-bZIP | MAFG | non-small cell lung cancer | | axonmedchem |
| MGL-3196 - VIA-3196 | Axon 2657
CAS [920509-32-6]
MF C17H12Cl2N6O4MW 435.22
Purity:
99%
Soluble in DMSO
Description
Oral, liver-targeted, selective thyroid hormone receptor β-agonist (EC50 value 0.21 µM for THR-β) that is being developed for the treatment of dyslipidemia. MGL-3196 is 28-fold selective for THR-β over THR-α in an in vitro functional coactivator recruitment assay.
KEYWORDS: MGL-3196 | supplier | THR-β agonist | VIA-3196 | MGL3196 | VIA3196 | CAS [920509-32-6] | Triiodothyronine | thyroid hormone receptor | THR | NR1A | nuclear receptor | dyslipidemia | HDL | LDL | cholesterol | cardiovascular | diabetes | hypercholesterolemic | | axonmedchem |
| JSH 23 | Axon 2349
CAS [749886-87-1]
MF C16H20N2MW 240.34
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Inhibitor of NF-κB transcription and nuclear translocation of p65 (IC50 value 7.1 µM for inhibition of LPS-induced NF-κB transcriptional activity) without affecting IκBα degradation, which is a very rare mode of action. JSH 23 inhibited not only LPS-induced expressions of tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6 and inducible nitric oxide synthase and cyclooxygenase-2 but also LPS-induced apoptosis of the RAW 264.7 cells. JSF 23 also inhibits NO production in LPS-stimulated macrophages RAW 264.7 (IC50 value 14.4 µM).
KEYWORDS: JSH 23 | supplier | NF-κB inhibitor | JSH23 | CAS [749886-87-1] | NF-κB | Inhibitor | p65 | IκB | inflammation | transcription factor | Pro-inflammatory | cytokine | LPS | IKK | RAW 264.7 | COX-2 | | axonmedchem |
| EVP 4593 | Axon 2080
CAS [545380-34-5]
MF C22H20N4OMW 356.42
Purity:
99%
Soluble in DMSO
Description
Potent NF-κB activation inhibitor (EC50: 9 nM); inhibits SOC pathway in HD neurons; exerts neuroprotective effects in transgenic HD flies and transgenic HD mouse neurons. EVP4593 was not active when tested in the IKK kinase assay
References
Certificates
Categories
Extra info
J Wu et al. Neuronal store-operated calcium entry pathway as a novel therapeutic target for Huntington's disease treatment. Chem. Biol. 2011, 18(6), 777-793.
M Tobe et al. A novel structural class of potent inhibitors of NF-kappa B activation: structure-activity relationships and biological effects of 6-aminoquinazoline derivatives. Bioorg. Med. Chem. 2003, 11, 3869–3878.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Immunology
Pain & Inflammation
Transcription Factors
NF-κB
L-Type
NF-κB
NF-κB activation inhibitor; inhibits SOC pathway
Chemical name
N4-(4-phenoxyphenethyl)quinazoline-4,6-diamine
Parent CAS No.
[545380-34-5]
Order
Size
Unit Price
Stock
10 mg
€110.00
In Stock | | axonmedchem |
| ML334 - LH601A | Axon 2641
CAS [1432500-66-7]
MF C26H26N2O5MW 446.50
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Activator of NRF2 signaling by inhibition of Keap1-NRF2 protein-protein interaction (PPI; IC50 value 1.6 - 2.3 µM in a fluorescence polarisation assay using Keap1 Kelch domain/NRF2-ETGE peptide; Kd value 1 μM to Keap1 Kelch domain). ML 334 stimulates NRF2 expression and nuclear translocation, and induces antioxidant response elements (ARE) and transcription of HO-1 and TRX1 proteins.
KEYWORDS: ML 334 | supplier | NRF2 acitivator | LH 601A | ML334 | LH601A | ML-334 | LH-601A | CAS [1432500-66-7] | DNA-RNA | NRF | Keap | Transcription Factor | Keap1-NRF2 | protein-protein interaction | Neurodegenerative | PPI | Kelch domain | expression | translocation | antioxidant response elements | HO-1 | TRX1 | | axonmedchem |
| BAY 11-7082 - BAY 11-7821 | Axon 2132
CAS [19542-67-7]
MF C10H9NO2SMW 207.25
Purity:
99%
Soluble in DMSO
Description
IKK inhibitor and broad-spectrum inhibitor with anti-inflammatory activity against multiple targets. BAY strongly suppressed the production of nitric oxide, prostaglandin E2, and TNF-α and reduced the translocation of p65, major subunit of nuclear factor-κB, and its upstream signaling events such as phosphorylation of IκBα, IKK, and Akt. In addition, BAY also inhibits the phosphorylation or activation of extracellular signal-related kinase, p38, TANK-binding protein, and JAK-2.
References
Certificates
Categories
Extra info
J Lee et al. BAY 11-7082 Is a Broad-Spectrum Inhibitor with Anti-Inflammatory Activity against Multiple Targets. Med. Inflammation, 2012, Article ID 416036.
M Ghashghaeinia et al. The NFĸB pathway inhibitors Bay 11-7082 and parthenolide induce programmed cell death in anucleated Erythrocytes. Cell Physiol. Biochem. 2011, 27, 45-54.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
Pain & Inflammation
Transcription Factors
NF-κB
EC 2.7.11.10
IKK
IKK inhibitor and anti-inflammatory
Chemical name
(E)-3-(p-tolylsulfonyl)acrylonitrile
Parent CAS No.
[19542-67-7]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| GSK 2033 | Axon 2363
CAS [1221277-90-2]
MF C29H28F3NO5S2MW 591.66
Purity:
100%
Soluble in DMSO
Description
The first potent cell-active LXR antagonist (IC50 value 31.6 nM for LXRβ binding). In intact cells stimulated with LXR agonist, GSK 2033 showed a dose-dependent reduction in the expression of the ATP-binding cassette transporter A1 (ABCA1) in THP-1 cells and SREBP-1c in HepG2 cells. A useful chemical probe to explore the cell biology of the LXR receptor.
KEYWORDS: GSK 2033 | supplier | LXR antagonist | GSK2033 | CAS [1221277-90-2] | Metabolism | LXR | Agonist | ATP-binding cassette transporter A1 | ABCA1 | nuclear receptor | NR | lipid | homeostasis | cholesterol | | axonmedchem |
| IMD-0354 | Axon 2725
CAS [978-62-1]
MF C15H8ClF6NO2MW 383.67
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
The IκB kinase-β (IKKβ or IKK-2) inhibitor IMD-0354 inhibited nuclear translocation of NF-κB induced by TNF-α; this attenuated myocardial reperfusion injury and preserved cardiac function after myocardial infarction. TNF-α-induced production of interleukin-1β and monocyte chemoattractant protein-1 was reduced significantly by IMD-0354. IMD-0354 restrained proliferation of mast cells with c-kit mutations and suppressed the growth of human breast cancer cells by arresting cell cycle at the G0-G1 phase and inducing apoptosis. May effectively prevent restenosis.
KEYWORD: IMD-0354 | supplier | IKK-2 inhibitor | IMD0354 | IMD 0354 | CAS [978-62-1] | IκB | IKK | Inhibitor | Enzymes | IκB kinase-β | NF-κB | TNF-α | restenosis | breast cancer | | axonmedchem |
| CRAC inhibitor 44 | Axon 1868
CAS [944917-72-0]
MF C22H19F2N3OSMW 411.47
Purity:
99%
Soluble in DMSO
Description
Potent and selective CRAC ion channel inhibitor (or blocker). The compound inhibits the activity of CRAC ion channels and the production of IL-2, IL-4, IL-5, IL-13, GM-CSF, TNF-α, and IFNγ
References
Certificates
Categories
Extra info
G Bohnert, S Chen and Y Xie. Preparation of vinyl phenyl compounds for treating inflammation and immune disorders. PCT Int. Appl. (2007), WO 2007087443 A2.
S Chen. Preparation of vinyl-aryl derivatives for inflammation and immune-related uses. PCT Int. Appl. (2009), WO 2009017831 A1.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Immunology
Pain & Inflammation
CRAC
L-Type
Potent and selective CRAC ion channel blocker
Chemical name
2,6-difluoro-N-(4-(4-methyl-1-(thiazol-2-yl)-1,2,5,6-tetrahydropyridin-3-yl)phenyl)benzamide
Parent CAS No.
[944917-72-0]
Order
Size
Unit Price
Stock
5 mg
€110.00
In Stock | | axonmedchem |
| T0901317 | Axon 2754
CAS [293754-55-9]
MF C17H12F9NO3SMW 481.33
Purity:
98%
Soluble in DMSO
Description
T0901317 is selective liver X receptor (LXR) agonist (EC50 value of 20 nM). Oral administration of T0901317 to mice and hamsters showed that LXR activated the coordinate expression of major fatty acid biosynthetic genes (lipogenesis) and increased plasma triglyceride and phospholipid levels in both species. Complementary studies in cell culture and animals suggested that the increase in plasma lipids occurs via LXR-mediated induction of the sterol regulatory element-binding protein 1 (SREBP-1) lipogenic program.
KEYWORDS: T0901317 | supplier | LXR agonist | T 0901317 | T-0901317 | CAS [293754-55-9] | Metabolism | LXR | Agonist | Receptors | Liver X Receptor | Lipogenesis | | axonmedchem |
| DY 268 | Axon 2561
CAS [1609564-75-1]
MF C30H32N4O5SMW 560.66
Purity:
100%
Soluble in DMSO
Description
Highly potent FXR antagonist with a promising in vitro profile (IC50 values 7.5 nM and 468.5 nM in FXR binding assay and cell-based FXR antagonistic assay, respectively). DY 268 shows no FXR agonistic activity nor cytotoxicity, making it an excellent chemical tool to elucidate the biological function of FXR.
KEYWORDS: DY 268 | supplier | FXR antagonist | DY268 | CAS [1609564-75-1] | Chenodeoxycholic acid | FXR | Antagonist | Nuclear | Farnesoid X Receptor | cholesterol | metabolism | | axonmedchem |
| WYE 672 | Axon 1991
CAS [1221265-37-7]
MF C23H17F3N2O2SMW 442.45
Purity:
99%
Soluble in DMSO
Description
A tissue selective liver X receptor (LXR) agonist; WYE672 showed potent binding affinity to LXRβ (IC50 = 53 nM), it had little binding affinity for LXRα (IC50 >1.0 μM)
References
Certificates
Categories
Extra info
B Hu et al. Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. J. Med. Chem. 2010, 53(8), 3296-3304.
T Jakobsson et al. Liver X receptor biology and pharmacology: new pathways, challenges and opportunities. Trends Pharmacol Sci. 2012, 33(7), 394-404.
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
NR1H
LXR
Liver X receptor (LXR) agonist
Chemical name
3-methyl-2-(3'-(methylsulfonyl)biphenyl-4-yl)-5-(trifluoromethyl)quinoxaline
Parent CAS No.
[1221265-37-7]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| SR 9243 | Axon 2598
CAS [1613028-81-1]
MF C31H32BrNO4S2MW 626.62
Purity:
99%
Soluble in DMSO
Description
LXR inverse agonist that induces LXR-corepressor interaction inhibiting the Warburg effect and lipogenesis in cancer cells by reducing glycolytic and lipogenic gene expression. SR 9243 induced apoptosis in tumors without inducing weight loss, hepatotoxicity, or inflammation. Moreover, SR 9243 may mediate tumor ‘‘unmasking’’ via downregulation of the immune-suppressive effects of LXR ligands within the tumor microenvironment. Close analogue of GSK 2033 (Axon 2363)
KEYWORDS: SR 9243 | supplier | LXR inverse agonist | SR9243 | CAS [1613028-81-1] | Metabolism | LXR | Inverse agonist | nuclear | Receptors | NR1H | Warburg effect | lipogenesis | cancer cells | glycolytic | lipogenic | gene expression | apoptosis | tumor unmasking | | axonmedchem |
| WAY 362450 - FXR 450 | XL 335 | Axon 1749
CAS [629664-81-9]
MF C25H24F2N2O3MW 438.47
Purity:
99%
Soluble in DMSO
Description
A highly potent, selective, and orally bioavailable farnesoid X receptor (FXR) agonist (EC50: 4 nM, eff=149%); potently induces luciferase reporter expression with an EC50 value of 16 nMpotently induces luciferase reporter expression with an EC50 value of 16 nM
References
Certificates
Categories
Extra info
B Flutt et al. Discovery of XL335 (WAY-362450), a Highly Potent, Selective, and Orally Active Agonist of the Farnesoid X Receptor (FXR). J. Med. Chem. 2009, 52(4), 904–907.
MJ Evans et al. A synthetic farnesoid X receptor (FXR) agonist promotes cholesterol lowering in models of dyslipidemia. Am. J. Physiol. Gastrointest. Liver Physiol. 2009, 296(3), G543-G552.
HB Hartman et al. Activation of farnesoid X receptor prevents atherosclerotic lesion formation in LDLR−/− and apoE−/− mice. J. Lipid Res. 2009, 50(6), 1090-1100.
S Zhang et al. Farnesoid X receptor agonist WAY-362450 attenuates liver inflammation and fibrosis in murine model of non-alcoholic steatohepatitis. J Hepatol. 2009, 51(2), 380-388.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
FXR
NR1H
Farnesoid X receptor (FXR) agonist
Chemical name
Isopropyl 3-(3,4-difluorobenzoyl)-1,1-dimethyl-1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate
Parent CAS No.
[629664-81-9]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| GW 3965 hydrochloride | Axon 1266
CAS [405911-17-3]
MF C33H31ClF3NO3.HClMW 618.51
Purity:
99%
Soluble in DMSO and Ethanol
Description
Selective and orally active liver X receptor (LXR) full agonist
References
Certificates
Categories
Extra info
N Mitro et al. The nuclear receptor LXR is a glucose sensor. Nature 2007, 445, 219-223.
JL Collins et al. Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. J. Med. Chem. 2002, 45 1963.
SB Joseph et al. Synthetic LXR ligand inhibits the development of atherosclerosis in mice. Proc. Natl. Acad. Sci. USA 2002, 99 7604.
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
NR1H
LXR
Liver X receptor agonist
Chemical name
(3-{3-[(2-Chloro-3-trifluoromethyl-benzyl)-(2,2-diphenyl-ethyl)-amino]-propoxy}-phenyl)-acetic acid hydrochloride
Parent CAS No.
[405911-09-3]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Pregabalin - PD 144723 | Axon 1823
CAS [148553-50-8]
MF C8H17NO2MW 159.23
Purity:
98%
Optical purity:
Optically pure
Soluble in water
Description
An analogue of γ-amino butyric acid (GABA) but inactive at GABA receptors. Pregabalin binds to the α2δ protein, an auxiliary protein associated with voltage-gated calcium channels in the central nervous system. Pregabalin reduces the synaptic release of several neurotransmitters by binding to α2δ subunits, possibly accounting for its actions in vivo to reduce neuronal excitability and seizures. Antiepileptic and analgesic.
References
Certificates
Categories
Extra info
CP Taylor et al. Pharmacology and mechanism of action of pregabalin: The calcium channel α2–δ (alpha2–delta) subunit as a target for antiepileptic drug discovery. Epilepsy Res. 2007, 73, 137–150.
Y Zhang et al. Development and validation of a direct enantiomeric separation of pregabalin to support isolated perfused rat kidney studies. J. Chrom. B. 2008, 875, 148–153.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Pain & Inflammation
α2δ subunit
Unclassified
Reduces synaptic signaling by binding to α2δ subunits
Chemical name
(S)-3-(aminomethyl)-5-methylhexanoic acid
Parent CAS No.
[148553-50-8]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| BAY K 8644, (S)-(-)- - BAY K8644, (-)- | Axon 1759
CAS [98625-26-4]
MF C16H15F3N2O4MW 356.30
Purity:
99%
Optical purity:
99% ee
Soluble in DMSO and Ethanol
Description
L-type Ca2+-channel activator with positive inotropic, vasoconstrictive and behavioral effects in vivo. The more active enantiomer (S) of Bay K8644 (Axon 1697), its opposite enantiomer, (R)-(+)-Bay-K8466 (Axon 1758) is also available.
KEYWORDS: (S)-(-)-BAY K 8644 | Supplier | Calcium (Ca2+) channel activator | BAY K8644, (-)- | BAY-K8644 | BAYK8644 | CAS [98625-26-4] | Calcium | Non Selective | Opener | Ion Channels | L-type | Ca2+-channel | positive inotropic | vasoconstrictive | | axonmedchem |
| BAY K 8644, (R)-(+)- - BAY K8644, (+)- | Axon 1758
CAS [98791-67-4]
MF C16H15F3N2O4MW 356.30
Purity:
100%
Optical purity:
99% ee
Soluble in DMSO and Ethanol
Description
L-type Ca2+-channel blocker with negative inotropic and vasodilatatory effects in vivo; (R)-Enantiomer showing opposite effects to the racemate (±)-Bay K8644 (Axon 1697) and (S)-(-)-Bay K8644 (Axon 1759).
KEYWORDS: (R)-(+)-BAY K 8644 | Calcium (Ca2+) channel activator | BAY K8644, (+)- | BAY-K8644 | BAYK8644 | CAS [98791-67-4] | Calcium | Non Selective | Blocker | Ion Channels | L-type | Ca2+-channel | negative inotropic | vasoconstrictive | | axonmedchem |
| Felodipine | Axon 1448
CAS [72509-76-3]
MF C18H19Cl2NO4MW 384.25
Purity:
99%
Soluble in DMSO
Description
Selective calcium channel blocker, a drug used to control hypertension
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Pain & Inflammation
Non Selective
L-Type
Ca2+ channel blocker
Chemical name
3,5-pyridinedicarboxylic acid, 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-, 3-ethyl-5-methylester
Parent CAS No.
[72509-76-3]
Order
Size
Unit Price
Stock
10 mg
€65.00
In Stock | | axonmedchem |
| Nifedipine | Axon 2068
CAS [21829-25-4]
MF C17H18N2O6MW 346.33
Purity:
99%
Soluble in DMSO
Description
A dihydropyridine calcium channel blocker (L-type), a drug used as an anti-anginal and anti-hypertensive
References
Certificates
Categories
Extra info
MJ Brown et al. Morbidity and mortality in patients randomised to double-blind treatment with a long-acting calcium-channel blocker or diuretic in the International Nifedipine GITS study: Intervention as (...). The Lancet, 2000, 356(9227), 366-372.
JH Weiss et al. The calcium channel blocker nifedipine attenuates slow excitatory amino acid neurotoxicity. Science, 1990, 247(4949), 1474-1477.
E Braunwald. Mechanism of action of calcium-channel-blocking agents. N. Engl. J. Med, 1982, 307(26), 1618.
W Vater et al. Pharmacology of 4-(2'-nitrophenyl)-2, 6-dimethyl-1, 4-dihydropyridine-3, 5-dicarboxylic acid dimethyl ester (Nifedipine, BAY a 1040). Arzneimittel-Forschung, 1972, 22(1), 1-14.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Pain & Inflammation
Non Selective
L-Type
Pfizer Licensed Products
Ca2+ channel blocker (L-type voltage gated)
Chemical name
dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[21829-25-4]
Order
Size
Unit Price
Stock
50 mg
€55.00
In Stock | | axonmedchem |
| Fantofarone - SR 33557 | Axon 2952
CAS [114432-13-2]
MF C31H38N2O5SMW 550.71
Purity:
98%
Soluble in DMSO
Recently added | | axonmedchem |
| SKF 96365 hydrochloride | Axon 1221
CAS [130495-35-1]
MF C22H26N2O3.HClMW 402.91
Purity:
99%
Soluble in water and DMSO
Description
Receptor-operated calcium channel blocker
References
Certificates
Categories
Extra info
Mernitt et al. SK&F96365, a novel inhibitor of receptor-mediated calcium entry. Biochem. J. 1990, 271, 515.
Leis et al. On the inhibition of prostanoid formation by SK&F 96365, a blocker of receptor-operated calcium entry. Br. J. Pharmacol. 1995, 114, 598.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Pain & Inflammation
Non Selective
Unclassified
Ca2+ channel blocker
Chemical name
1-{2-(4-Methoxy-phenyl)-2-[3-(4-methoxy-phenyl)-propoxy]-ethyl}-1H-imidazole hydrochloride
Parent CAS No.
[162849-90-3]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| BMS 345541 | Axon 1731
CAS [547757-23-3]
MF C14H17N5.HClMW 291.78
Purity:
98%
Soluble in water and DMSO
Description
A cell-permeable and highly selective IKB kinase (IKK) inhibitor, binds at allosteric site of the enzyme; blocks NF-kB-dependent transcription in mice; Displays ~10-fold greater selectivity at IKK-2 over IKK-1.
KEYWORDS: BMS 345541 | supplier | IKK inhibitor | BMS345541 | BMS-345541 | CAS [547757-23-3] | [445430-58-0] | IκB | IKK | IKB kinase | NF-kB-dependent transcription | cell-permeable | allosteric | IKK-2 | IKK-1 | | axonmedchem |
| PHA 408 | Axon 1651
CAS [503555-55-3]
MF C29H27ClFN7O2MW 560.02
Purity:
99%
Soluble in DMSO
Description
Potent, highly selective and ATP-competitive IKB kinase-2 (IKK-2) inhibitor (IC50: 40 nM), which binds IKK-2 tightly with a relatively slow off rate; highly recommended tool to investigate the mechanisms by which IKK-2 regulates NF-KB signaling
References
Certificates
Categories
Extra info
G Mbalaviele et al. A novel, highly selective, tight binding IkB kinase-2 (IKK-2) inhibitor: a tool to correlate IKK-2 activity to the fate and functions of the components of the nuclear factor-kB pathway (...). J. Ph. Exp. Ther. 2009, 329(1), 14-25.
CD Sommers et al. Novel tight-binding inhibitory factor-kB kinase (IKK-2) inhibitors demonstrate target-specific anti-inflammatory activities in cellular assays (...). J. Pharmacol. Exp. Ther. 2009, 330(2), 377-388.
S Rajendrasozhan et al. Anti-inflammatory effect of a selective IkB kinase-beta inhibitor in rat lung in response to LPS and cigarette smoke. Pulm. Pharmacol. Ther. 2010, 23(3), 172-181.
S Mathialagan et al. Expression, purification and functional characterization of IkB kinase-2 (IKK-2) mutants. Protein Expr. Purif. 2010, 72(2), 254-261.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
Pain & Inflammation
Transcription Factors
NF-κB
EC 2.7.11.10
IKK
IKK-2 inhibitor
Chemical name
8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
Parent CAS No.
[503555-55-3]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| LXR 623 - WAY 252623 | Axon 2357
CAS [875787-07-8]
MF C21H12ClF5N2MW 422.78
Purity:
99%
Soluble in DMSO
Description
Partial agonist of Liver X Receptor (LXR; IC50 value 179 nM and 24 nM for LXRα- and LXRβ-binding, respectively. EC50 values 6.66 μM and 3.67 μM for Huh-7 human hepatoma cell based Gal4 LXRα and LXRβ transactivation essays respectively). Despite its partial agonism in transactivation essays, LXR 623 exhibits full agonism in THP-1 cells with respect to increasing ABCA1 gene expression and on cholesterol efflux in THP-1 foam cells. In vivo, LXR 623 lowers LDL cholesterol in primates, is lipid neutral in hamster, and reduces atherosclerosis in mouse.
References
Certificates
Categories
Extra info
C. Giannarelli et al. Synergistic effect of liver X receptor activation and simvastatin on plaque regression and stabilization: an magnetic resonance imaging study in a model of advanced atherosclerosis. Eur. Heart J. 2012, 33, 264-273.
J. Wrobel et al. Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. J. Med. Chem. 2008, 51, 7161-7168.
E.M. Quinet et al. LXR ligand lowers LDL cholesterol in primates, is lipid neutral in hamster, and reduces atherosclerosis in mouse. J. Lipid Res. 2009, 50, 2358-2370.
E.A. DiBlasio-Smith et al. Discovery and implementation of transcriptional biomarkers of synthetic LXR agonists in peripheral blood cells. J. Transl. Med. 2008, 6, 59.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Diabetes & Metabolism
NR1H
LXR
Partial agonist of Liver X Receptor
Chemical name
2-(2-chloro-4-fluorobenzyl)-3-(4-fluorophenyl)-7-(trifluoromethyl)-2H-indazole
Parent CAS No.
[875787-07-8]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| BX 795 | Axon 1390
CAS [702675-74-9]
MF C23H26IN7O2SMW 591.47
Purity:
98%
Soluble in DMSO
Description
BX 795 was initially developed as a PDPK1 inhibitor. Recent study highlighted on its bioactivitiy as a potent and relatively specific inhibitor of TBK1 and closely related IKKε, with IC50 values to be 6, 41, and 111 nM for TBK1, IKKε and PDPK1 respectively.
KEYWORDS: BX 795 | supplier | PDK1/TBK1 inhibitor | BX795 | BX-795 | CAS [702675-74-9] | Phosphatidylinositol | IKK | PDPK | PDK1 | TBK | TBK1 | IKK-epsilon | | axonmedchem |
| Crizotinib, (S)- | Axon 2296
CAS [1374356-45-2]
MF C21H22Cl2FN5OMW 450.34
Purity:
99%
Optical purity:
98.5 % e.e.
Soluble in DMSO
Description
(S)-Crizotinib is a selective inhibitor of the human mutT homologue MTH1 (also known as NUDT1; IC50 value 72 nM; Kd value 48 nM). MTH1 inhibition by (S)-Crizotinib induced an increase in DNA single-strand breaks, activated DNA repair in human colon carcinoma cells, and effectively suppressed tumor growth in animal models. It is the opposite (S)-enantiomer of (R)-Crizotinib (PF-02341066, Axon 1660), which is a ALK/MET inhibitor. MTH1 (human mutT homologue, or NUDT1) has been implicated in aiding RAS-transformed cells to overcome oncogene-induced senescence by preventing reactive oxygen species (ROS)-induced DNA damage.
References
Certificates
Categories
Extra info
K.V.M. Huber et al. Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. Nature. 2014, 508, 222-227.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
DNA-damage Response
MTH1
EC 3.6.1.56
MTH1 inhibitor
Chemical name
(S)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine
Parent CAS No.
[1374356-45-2]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| PS 47 | Axon 1664
CAS [1180676-33-8]
MF C17H15ClO2MW 286.75
Purity:
99%
Soluble in DMSO
Description
Inactive E-isomer of the allosteric activator of phosphoinositide-dependent protein kinase 1 (PDPK1 or PDK1) PS 48 (Axon 1659). PS 47 can be used as a negative control when used in combination with PS 48.
KEYWORDS: PS 47 | supplier | PDK1 negative control | PS47 | CAS [1180676-33-8] | Phosphatidylinositol | PDPK1 | Inhibitor | allosteric | negative control | inactive isomer | phosphoinositide-dependent protein kinase 1 | PS 48 | PS48 | | axonmedchem |
| PX 20350 - FXR agonist Cpd 22 | Axon 2152
CAS [1198085-23-2]
MF C28H22Cl2F3N3O4MW 592.39
Purity:
99%
Soluble in DMSO
Description
Potent farnesoid X receptor (FXR) agonist with enhanced affinity and efficacy (12 nM and 109% (compared to GW 4064)) in FXR FRET assay and full length FXR direct reporter (DR) assay (6 nM vs 30 nM for GW 4064). Cpd 22 showed a linear dose-dependent reduction in total plasma triglycerides and total plasma cholesterol.
References
Certificates
Categories
Extra info
U. Abel et al. Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists. Bioorg. Med. Chem. Lett. 2010, 20, 4911–4917.
U. Deuschle et al. FXR controls the tumor suppressor NDRG2 and FXR agonists reduce liver tumor growth and metastasis in an orthotopic mouse xenograft model. PLoS One. 2012, 7, e43044.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
FXR
NR1H
Potent farnesoid X receptor (FXR) agonist
Chemical name
4-(((6-((5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl)methoxy)-2-(trifluoromethyl)pyridin-3-yl)(methyl)amino)methyl)benzoic acid
Parent CAS No.
[1198085-23-2]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| L67 | Axon 2549
CAS [325970-71-6]
MF C16H14Br2N4O4MW 486.11
Purity:
99%
Soluble in DMSO
Description
Cytotoxic inhibitor of DNA ligase I and III (IC50 values 10 μM each) that binds to the DBD of hLigI, hence leading to inhibition of DNA binding and ligation and specifically sensitizes cancer cells to DNA damage. Breast cancer cell lines with acquired resistance to antiestrogen therapeutics are hypersensitive to a combination of L67 and PARP inhibitor ABT 888 (Axon 1593).
KEYWORDS: L67 | supplier | DNA ligase inhibitor | L-67 | CAS [325970-71-6] | DNA-RNA | DNA-ligase | Inhibitor | cytotoxic | breast | cancer | replication | double-strand break | DSB | DNA damage | NHEJ | ATP-dependent | | axonmedchem |
| OSU 03012 | Axon 2525
CAS [742112-33-0]
MF C26H19F3N4OMW 460.45
Purity:
99%
Soluble in DMSO
Description
ATP-competitive PDK-1 inhibitor (IC50 value 5 μM for both PDK-1/PDPK1) that inhibits the growth of thyroid, prostate and breast cancer xenografts in vivo. A Celecoxib (Axon 1919) derivative that inhibits PAK phosphorylation and cell proliferation with reduced Akt phosphorylation by PDK1, without inhibition of cycloogygenases. Moreover, overexpression of constitutively active forms of PDK-1 and Akt partially protected OSU-03012-induced apoptosis.
KEYWORDS: OSU 03012 | supplier | PDK-1 inhibitor | OSU03012 | CAS [742112-33-0] | Phosphatidylinositol | PDPK | PAK | Akt | apoptosis | prostate | breast | thyroid | cancer | proliferation | p70S6 | p21 | PKC | | axonmedchem |
| PDK1 inhibitor 2610 | Axon 2610
CAS [N.A.]
MF C25H15N5.HClMW 421.88
Purity:
99%
Soluble in water and DMSO
Description
Potent, ATP-competitive and selective dual PI3K and PDPK1 inhibitor (IC50 values 34 nM and 94 nM for PDK1 and p-T308-PKB inhibition, respectively. Also inhibits PI3K p110α, p110β, p110δ, and p110γ (IC50 values 64 nM, 432 nM , 98 nM, and 67 nM, respectively).
Axon 2610 is a close analogue of NVP-BAG956 (Axon 1282)
KEYWORDS: PDK1 inhibitor 2610 | supplier | PI3K/PDK1 inhibitor | CAS [853909-77-0] | Phosphatidylinositol | PI3K | PDPK | Inhibitor | PKB | Akt | p110 | Oncology | PIP3 | Novartis | | axonmedchem |
| SCR7 pyrazine | Axon 2531
CAS [14892-97-8]
MF C18H12N4OSMW 332.38
Purity:
99%
Soluble in DMSO
Description
DNA ligase IV mediated inhibitor of NHEJ (non-homologous end joining) that increases the efficiency of homology-directed repair for CRISPR-Cas9-induced precise gene editing in mammalian cells up to 19-fold.
Note | | axonmedchem |
| Taselisib - GDC 0032 | RG 7604 | Axon 2927
CAS [1282512-48-4]
MF C24H28N8O2MW 460.53
Purity:
99%
Soluble in DMSO
Description
Taselisib is a β-sparing PI3K inhibitor with Ki values of 0.29, 0.12 and 0.97 nM for PI3Kα, PI3Kδ and PI3Kγ, respectively. Moreover, Taselisib showed improved unbound drug exposure and effectively suppressed growth of tumors in a mouse xenograft model at low drug dose levels.
KEYWORDS: Taselisib | supplier | PI3K inhibitor | GDC 0032 | RG 7604 | GDC0032 | GDC-0032 | RG7604 | RG-7604 | CAS [1282512-48-4] | Phosphatidylinositol | PI3K | Inhibitor | Enzymes | Antitumor | | axonmedchem |