| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| BH3I 1 - BHI 1 | Axon 1828
CAS [300817-68-9]
MF C15H14BrNO3S2MW 400.31
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Cell permeable antitumor agent targeting Bcl-2 family protein, more specifically as Bcl-xL antagonist; apoptosis inducer, inducing a dose- and time-dependent apoptosis in H460 and H1792 cells
References
Certificates
Categories
Extra info
W Roa et al. Enhancement of radiation sensitivity with BH3I-1 in non-small cell lung cancer. Clin. Invest. Med. 2005, 28(2), 55-63.
S Shangary and DE Johnson. Recent advances in the development of anticancer agents targeting cell death inhibitors in the Bcl-2 protein family. Leukemia 2003, 17, 1470–1481.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Bcl
Inhibitor of Bcl-2 family protein
Chemical name
2-(5-(4-bromobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)-3-methylbutanoic acid
Parent CAS No.
[300817-68-9]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| Erastin | Axon 1825
CAS [571203-78-6]
MF C30H31ClN4O4MW 547.04
Purity:
99%
Soluble in DMSO
Description
An anti-tumor agent with RAS-selective lethality. Erastin binds to mitochondrial voltage-dependent anion channels (VDAC) proteins, more specifically on VDAC2 and alters its gating; induce non-apoptotic cell death selectively in some tumour cells harbouring activating mutations in the RAS-RAF-MEK pathway
References
Certificates
Categories
Extra info
N Yagoda et al. RAS–RAF–MEK-dependent oxidative cell death involving voltage-dependent anion channels. Nature 2007, 447, 865-869.
Citation: JF Foley, Selective Killing. Sci. STKE 2007, 391, p. tw212.
E imamura et al. Mitochondrial voltage-dependent anion channels (VDACs) as novel pharmacological targets for anti-cancer agents. J. Bioenerg. Biomembr. 2008, 40(3), 213-217.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
VDAC2
Unclassified
VDAC2 modulator
Chemical name
4(3H)-Quinazolinone, 2-[1-[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-
Parent CAS No.
[571203-78-6]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| YM 155 | Axon 1639
CAS [781661-94-7]
MF C20H19BrN4O3MW 443.29
Purity:
98%
Soluble in DMSO
Description
Small molecule survivin suppresant or inhibitor; YM155 suppressed expression of survivin and induced apoptosis in p53-deficient human HRPC cell lines at 10 nmol/L
References
Certificates
Categories
Extra info
A Kita et al. Survivin suppressant: a promising target for cancer therapy and pharmacological profiles of YM155. Nippon Yakurigaku Zasshi 2010, 136(4), 198-203.
T Iwasa et al. Marked anti-tumour activity of the combination of YM155, a novel survivin suppressant, and platinum-based drugs. Br. J. Cancer 2010, 103(1),36-42.
T Nakahara et al. YM155, a Novel Small-Molecule Survivin Suppressant, Induces Regression of Established Human Hormone-Refractory Prostate Tumor Xenografts. Cancer Res. 2007, 67, 8014-8021.
R Gonzalez et al. A phase II study of YM155, a novel survivin suppressant, administered by 168 hour continuous infusion in patients with unresectable stage III or stage IV melanoma. J. Clin. Oncol. 2007, 25(18S), 8538.
T Satoh et al. Phase I Study of YM155, a Novel Survivin Suppressant, in Patients with Advanced Solid Tumors. Clin. Cancer Res. 2009, 15, 3872.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Ubiquitin
IAP
Survivin suppressant
Chemical name
1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazol-3-ium bromide
Parent CAS No.
[N.A.]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| SR 3576 | Axon 2365
CAS [1164153-22-3]
MF C27H27N5O5MW 501.53
Purity:
99%
Soluble in DMSO
Description
Very potent JNK3 inhibitor (IC50 value 7 nM) with >2800-fold selectivity over p38 (p38 IC50 value >20 μm) and a cell-based potency of ca. 1 μM.
References
Certificates
Categories
Extra info
T. Kamenecka et al. Structure-activity relationships and X-ray structures describing the selectivity of aminopyrazole inhibitors for c-Jun N-terminal kinase 3 (JNK3) over p38. J. Biol. Chem. 2009, 284, 12853-12861.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Immunology
Pain & Inflammation
MAPK (JNK)
p53-Tumor Suppression
NF-κB
MAPK
EC 2.7.11.24
Very potent JNK3 inhibitor with >2800-fold selectivity over p38
Chemical name
3-(4-(3-m-tolylureido)-1H-pyrazol-1-yl)-N-(3,4,5-trimethoxyphenyl)benzamide
Parent CAS No.
[1164153-22-3]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| JNK-IN-8 | Axon 2361
CAS [1410880-22-6]
MF C29H29N7O2MW 507.59
Purity:
98%
Soluble in DMSO
Description
Remarkably potent and selective covalent inhibitor of JNK (IC50 values 4.67 nM, 18.7 nM, and 0.98nM for JNK1/2/3, respectively). JNK-IN-8 inhibits phosphorylation of c-Jun, a direct substrate of JNK, in cells exposed to submicromolar drug in a manner that depends on covalent modification of the conserved cysteine residue (EC50 values 486 nM and 338 nM for inhibition of c-Jun phosphorylation in HeLa and A375 cells, respectively).
Useful as a pharmacological probe of JNK-dependent signal transduction
References
Certificates
Categories
Extra info
T. Zhang et al. Discovery of potent and selective covalent inhibitors of JNK. Chem. Biol. 2012, 19, 140-154.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
CNS
Immunology
Pain & Inflammation
MAPK (JNK)
p53-Tumor Suppression
NF-κB
MAPK
EC 2.7.11.24
Remarkably potent and selective covalent inhibitor of JNK
Chemical name
(E)-3-(4-(dimethylamino)but-2-enamido)-N-(3-methyl-4-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl)benzamide
Parent CAS No.
[1410880-22-6]
Order
Size
Unit Price
Stock
5 mg
€120.00
In Stock | | axonmedchem |
| AS 602801 - Bentamapimod | Axon 2002
CAS [848344-36-5]
MF C25H23N5O2SMW 457.55
Purity:
98%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent, orally active and selective Jun kinase (JNK) inhibitor, which inhibited JNK1, JNK2 and JNK3 with IC50 values of 80, 90 and 230 nM respectively. It blocked T-lymphocyte proliferation and induced apoptosis
References
Certificates
Categories
Extra info
S Halazy. Designing heterocyclic selective kinase inhibitors: from concept to new drug candidates. ARKIVOC 2006 (vii) 496-508.
C Chiara Ferrandi et al. Characterization of immune cell subsets during the active phase of multiple sclerosis reveals disease and c-Jun N-terminal kinase pathway biomarkers. Mult. Scler. J. 2011, 17(1), 43-56.
SS Bhagwat. Chapter 17 MAP Kinase Inhibitors in Inflammation and Autoimmune Disorders. Ann. Rep. Med. Chem. 2007, 42, 265-278.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Immunology
Pain & Inflammation
MAPK (JNK)
p53-Tumor Suppression
NF-κB
MAPK
EC 2.7.11.24
JNK inhibitor, which inhibited JNK1, JNK2 and JNK3
Chemical name
2-(benzo[d]thiazol-2-yl)-2-(2-(4-(morpholinomethyl)benzyloxy)pyrimidin-4-yl)acetonitrile
Parent CAS No.
[848344-36-5]
Order
Size
Unit Price
Stock
5 mg
€120.00
In Stock | | axonmedchem |
| AEG 3482 | Axon 1291
CAS [63735-71-7]
MF C10H8N4O2S2MW 280.33
Purity:
99%
Soluble in DMSO
Description
Inhibitor of JNK signaling
References
Certificates
Categories
Extra info
AH Salehi et al. AEG3482 is an antiapoptotic compound that inhibits Jun kinase activity and cell death through induced expression of heat shock protein 70. Chem. Biol. 2006, 13, 213.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Immunology
Pain & Inflammation
MAPK (JNK)
p53-Tumor Suppression
NF-κB
MAPK
EC 2.7.11.24
JNK inhibitor
Chemical name
6-Phenyl-imidazo[2,1-b][1,3,4]thiadiazole-2-sulfonic acid amide
Parent CAS No.
[63735-71-7]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| CC-401 | Axon 2025
CAS [395104-30-0]
MF C22H24N6OMW 388.47
Purity:
99%
Soluble in DMSO and Ethanol
Description
A second generation ATP-competitive c-Jun N terminal kinase (JNK) inhibitor with potential antineoplastic activity.
Keywords: CC-401 | supplier | JNK inhibitor | CC401 | CC 401 | CAS [395104-30-0] | MAPK | MAPK (JNK) | Inhibitor | Enzymes | | axonmedchem |
| ZCL 278 | Axon 2138
CAS [587841-73-4]
MF C21H19BrClN5O4S2MW 584.89
Purity:
98%
Soluble in DMSO
Description
Selective Cdc42 GTPase inhibitor. ZCL 278 specifically targets Cdc42–ITSN interaction and inhibits Cdc42-mediated cellular processes, thus providing a powerful tool for research of Cdc42 subclass of Rho GTPases in human pathogenesis. ZCL 278 reduces the perinuclear accumulation of active Cdc42 in contrast to NSC 23766 (Axon 1578), a selective Rac inhibitor.
References
Certificates
Categories
Extra info
A Friesland et al. Small molecule targeting Cdc42–intersectin interaction disrupts Golgi origanization and suppresses cell motility. Proc. Natl Acad. Sci. USA. 2013, 110, 1261-1266.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Stem Cell
Cdc42
p53-Tumor Suppression
EC 3.6.5.2
Cdc42 GTPase inhibitor, targeting Cdc42–ITSN interaction
Chemical name
2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(4,6-dimethylpyrimidin-2-yl)sulfamoyl)phenylcarbamothioyl)acetamide
Parent CAS No.
[587841-73-4]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| BXL 628 - Elocalcitol | RO 26-9228 | Axon 1676
CAS [199798-84-0]
MF C29H43FO2MW 442.65
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO and Ethanol
Description
A vitamin D3 analog having agonistic activities at vitamin D receptor (VDR); BXL-628 inhibits prostate cell growth and RhoA/Rho-kinase signaling, a calcium sensitizing pathway; having anti-proliferative and anti-inflammatory properties in benign prostatic hyperplasia (BPH) treatment
References
Certificates
Categories
Extra info
C Crescioli et al. Inhibition of prostate cell growth by BXL-628, a calcitriol analogue selected for a phase II clinical trial in patients with benign prostate hyperplasia. Eur. J. Endocrinol. 2004, 150(4), 591-603.
E Colli et al. BXL628, a novel vitamin D3 analog arrests prostate growth in patients with benign prostatic hyperplasia: a randomized clinical trial. Eur Urol. 2006, 49(1), 82-86.
A Morelli et al. BXL-628, a vitamin D receptor agonist effective in benign prostatic hyperplasia treatment, prevents RhoA activation and inhibits RhoA/Rho kinase signaling in rat and human bladder. Prostate. 2007, 67(3), 234-247.
G Penna et al. The vitamin D receptor agonist elocalcitol inhibits IL-8-dependent benign prostatic hyperplasia stromal cell proliferation and inflammatory response by targeting the RhoA/Rho kinase and NF-kappaB pathways. Prostate. 2009, 69(5), 480-493.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Pain & Inflammation
Stem Cell
Endocrinology
VDR
NR1I
Vitamin D receptor (VDR) agonist
Chemical name
(1R,5S,Z)-3-((E)-2-((3aS,7aS)-3-((S,E)-6-ethyl-6-hydroxyoct-4-en-2-yl)-3a-methyl-3a,4,5,6-tetrahydro-1H-inden-7(7aH)-ylidene)ethylidene)-5-fluoro-4-methylenecyclohexanol
Parent CAS No.
[199798-84-0]
Order
Size
Unit Price
Stock
2 mg
€165.00
In Stock | | axonmedchem |
| A 83-01 | Axon 1421
CAS [909910-43-6]
MF C25H19N5SMW 421.52
Purity:
99%
Soluble in DMSO
Description
Potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 and its relatives ALK4 and ALK7 (IC50 to be 12, 45 and 7.5 nM respectively). A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β, but had no effect on BMP signaling; Used to generate rat and human iPS cells towards a mouse ES cell like self-renewal state.
*Note: A 83-01 is found to decompose to A 77-01 (Axon 1744) in solution slowly. Hence freshly prepared solution is highly recommended and otherwise, its stock solution in DMSO needs to be stored <-20 °C (not longer than 1 month).
KEYWORDS: A 83-01 | supplier | ALK5 inhibitor | A83-01 | A8301 | CAS [909910-43-6] | TGF-β | TGF-βR | Antagonist | ALK4 | ALK7 | Smad | signaling | epithelial | mesenchymal | transition | iPS | self-renewal | | axonmedchem |
| Tacalcitol - PRI 2191 | 1α,24-Dihydroxycholecalciferol | Axon 2516
CAS [57333-96-7]
MF C27H44O3MW 416.64
Purity:
98%
Soluble in DMSO
Description
Vitamine D receptor agonist (EC50 value 7 nM for VDR) and metabolite of vitamin D3 with a higher antitumor and lower calcemic activity as well as lower toxicity than Calcitriol. Tacalcitol inhibits proliferation and induces differentiation of keratinocytes. Tacalcitol (PRI 2191) promotes normal bone formation, and is a well-known inhibitor of chemical mediated inflammatory changes including dermal cellular infiltration and epidermal hyperplasia, used to treat T cell-mediated inflammatory skin diseases such as psoriasis, prurigo and vitiligo. PRI2191 enhances the antiproliferative effect of Imatinib (Axon 1394) on HL-60 cells.
Note: | | axonmedchem |
| BAY K 8644 - BAY K 8644, (±)- | Axon 1697
CAS [71145-03-4]
MF C16H15F3N2O4MW 356.30
Purity:
99%
Soluble in DMSO and Ethanol
Description
A L-type calcium channel activator that facilitates Ca2+ influx specifically at voltage-gated Ca2+ channels, thereby causing vasoconstrictor and positive inotropic effects.
It is used primarily as a research tool. Bay-K8644 in combination of BIX-01294 (Axon 1692) enables reprogramming of Oct4/Klf4-transduced mouse embryonic fibroblasts.
Its two enantiomers, (R)-(+)-BAY-K8644 (Axon 1758) and (S)-(-)-BAY-K8466 (Axon 1759), are also available.
KEYWORDS: BAY K 8644 | Ca channel activator | BAY K 8644, (±)- | BAYK8644 | K8644 | CAS [71145-03-4] | Calcium | Non Selective | Opener | Ion Channels | L-type | Ca2+-channel | positive inotropic | vasoconstrictive | | axonmedchem |
| NSC 23766 | Axon 1578
CAS [1177865-17-6]
MF C24H35N7.3HClMW 530.96
Purity:
99%
Soluble in water and DMSO
Description
A cell-permeable, reversible, and selective Rac1 inhibitor; inhibiting Rac1 activation by the Rac-specific GEFs TrioN and Tiam 1 (IC50 = 50 μM) without affecting the closely related GTPases, Cdc42, and RhoA activation.A useful tool for studying the Rac-mediated cellular functions and for modulating pathological conditions in which Rac-deregulation may play a role.
KEYWORDS: NSC 23766 | supplier | Rac1-GEF inhibitor | NSC23766 HCl | CAS [1177865-17-6] | [733767-34-5] | Cytoskeleton | Rac | Rho | GTPase | GEFs | TrioN | Tiam1 | hematopoietic | stem cell | HSC | leukemia | | axonmedchem |
| Doxercalciferol - Hectorol | TSA 840 | Axon 1746
CAS [54573-75-0]
MF C28H44O2MW 412.65
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
A vitamin D2 analog having agonistic activities at vitamin D receptor (VDR)
References
Certificates
Categories
Extra info
JA Di Paolo et al. Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis. Nat. Chem. Biol. 2011, 7(1), 41-50.
Y Lou et al. Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. J. Med. Chem. 2012, 55(10), 4539-4350.
SL Tamn et al. Targeting the SYK–BTK axis for the treatment of immunological and hematological disorders: Recent progress and therapeutic perspectives. Pharmacol. & Ther. 2013, 138(2), 294-309.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Endocrinology
VDR
NR1I
Vitamin D2 analog, VDR agonist
Chemical name
(1R,3S,Z)-5-((E)-2-((1R,3aS,7aR)-1-((2R,5R,E)-5,6-dimethylhept-3-en-2-yl)-7a-methyldihydro-1H-inden-4(2H,5H,6H,7H,7aH)-ylidene)ethylidene)-4-methylenecyclohexane-1,3-diol
Parent CAS No.
[54573-75-0]
Order
Size
Unit Price
Stock
2 mg
€105.00
In Stock | | axonmedchem |
| Akt Inhibitor VIII - Akti-1/2 | Axon 2540
CAS [612847-09-3]
MF C34H29N7OMW 551.64
Purity:
98%
Soluble in 0.1N HCl(aq) and DMSO
Description
Non-ATP-competitive inhibitor of Akt isoforms 1 and 2 (IC50 values 58 nM and 210 nM for Akt1 and Akt2, respectively). Moreover, the Akt inhibitor efficiently inhibits Ca2+/CaM-dependent protein kinase (CaMKIα) activity (IC50 value 3.99 μM) and prevents TCDD induced nuclear translocation of aryl hydrocarbon receptor (AhR) in MCF-7 cells. Akti-1/2 inhibitory effects towards CaMKIα and TCDD-induced EROD activity in function of Akti-1/2 concentrations were quite similar (IC50 ± SD, 3.99 ± 0.82 μM and 5.86 ± 1.85 μM, respectively).
KEYWORDS: Akt Inhibitor VIII | supplier | Akt inhibitor | Akti-1/2 | compound8 | inhibitorVIII | CAS [612847-09-3] | Phosphatidylinositol | Akt | PI3K | PKB | calcium | Ca2+/CaM-dependent protein kinase | CaMKIα | aryl hydrocarbon receptor | AhR | TCDD | | axonmedchem |
| JNJ 10191584 | Axon 1307
CAS [73903-17-0]
MF C13H15ClN4OMW 278.74
Purity:
99%
Soluble in DMSO
Description
Selective silent histamine H4 receptor antagonist, orally active
References
Certificates
Categories
Extra info
Csaba Varga et al. Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat. Eur. J. Pharmacol. 2005, 522(1-3), 130-138.
Certificate of Analysis
Material Safety Data Sheet
CNS
Immunology
Pain & Inflammation
H4
A18
H4 antagonist
Chemical name
(6-Chloro-1H-benzoimidazol-2-yl)-(4-methyl-piperazin-1-yl)-methanone
Parent CAS No.
[73903-17-0]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| LY 2584702 tosylate | Axon 2464
CAS [1082949-68-5]
MF C21H19F4N7.C7H8O3SMW 617.62
Purity:
98%
Soluble in DMSO
Description
Oral, selective ATP-competitive inhibitor of p70 S6 kinase (S6K1; IC50 value 4 nM) with significant synergistic activity with Erlotinib (Axon 1128) and Everolimus. LY2584702 is selective against 83 other kinases as determined by a ubiquitin kinase panel, and 45 cell surface markers as determined by a CEREP mini panel.
KEYWORDS: LY 2584702 tosylate | supplier | S6K1 inhibitor | LY 2779964 | LY2584702 | LY2779964 | CAS [1082949-68-5] | [1082949-67-4] | (Ribosomal proteins) | p70-RSK | Inhibitor | p70S6K | PI3K | mTOR | Akt | ribosomal | cancer | Phase I | trial | ATP-competitive | | axonmedchem |
| BIX 01294 trihydrochloride | Axon 1692
CAS [935693-62-2]
MF C28H38N6O2.3HClMW 600.02
Purity:
99%
Soluble in water and DMSO
Description
G9a-like protein and G9a histone lysine methyltransferase (HMTase) inhibitor; Recently, BIX-01294 and RG108 (Axon 1691) have been reported to enhance the efficiency of iPS cell generation
*Promotion | | axonmedchem |
| VUF 10460 | Axon 2126
CAS [1028327-66-3]
MF C15H19N5MW 269.34
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Selective histamine H4 receptor agonist.
References
Certificates
Categories
Extra info
M Adami et al. Effects of Histamine H4 Receptor Ligands in a Mouse Model of Gastric Ulceration. Pharmacology, 2012, 89(5-6), 287-294.
G Coruzzi et al. Selective histamine H3 and H4 receptor agonists exert opposite effects against the gastric lesions induced by HCl in the rat stomach. Eur. J. Pharmacol. 2011, 669(1), 121-127.
Certificate of Analysis
Material Safety Data Sheet
CNS
Immunology
Pain & Inflammation
H4
A18
H4 agonist
Chemical name
4-(4-methylpiperazin-1-yl)-6-phenylpyrimidin-2-amine
Parent CAS No.
[1028327-66-3]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| CM-272 | Axon 2812
CAS [1846570-31-7]
MF C28H38N4O3MW 478.63
Purity:
98%
Soluble in 0.1N HCl(aq) and DMSO
Recently added | | axonmedchem |
| BAY-598 | Axon 2635
CAS [1906919-67-2]
MF C22H20Cl2F2N6O3MW 525.34
Purity:
98%
Optical purity:
99% e.e.
Soluble in DMSO
Description
BAY-598 is a potent, selective, and cell-active, substrate-competitive inhibitor of SMYD2 (IC50 values of 27 nM and 58 nM for biochemical and cellular activity, respectively). BAY-598 also shows PAR1 antagonism, but there is a greater than 50-fold selectivity for SMYD2 relative to PAR1.
KEYWORDS: BAY-598 | supplier | SMYD2 inhibitor | BAY598 | BAY 598 | CAS [1906919-67-2] | Histone | HMTase | Inhibitor | Enzymes | SET | MYND | Protein Methylation | Chemical Probe | Apoptosis | Protein Lysine Methyltransferase | SET and MYND Domain Containing Protein 2 | | axonmedchem |
| GSK 2110183 hydrochloride - Afuresertib hydrochloride | Axon 2460
CAS [1047645-82-8]
MF C18H17Cl2FN4OS.HClMW 463.78
Purity:
99%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Potent, reversible, selective, and orally bioavailable inhibitor of the Akt kinases (Ki values 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively), with some inhibitory effect on PKA and PKG1a. GSK2110183 preferentially inhibits the proliferation of human cancer cell lines with Akt pathway activation, and various cell lines derived from hematologic malignancies, in an ATP-competitive manner and with a minimal effect on glucose homeostasis.
References
Certificates
Categories
Extra info
M. Dumble et al. Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor. PLoS One. 2014 Jun 30;9(6):e100880.
A. Spencer et al. The novel AKT inhibitor afuresertib shows favorable safety, pharmacokinetics, and clinical activity in multiple myeloma. Blood. 2014 Oct 2;124(14):2190-5.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Akt
PI3K-Akt-mTOR
EC 2.7.11.1
Potent, reversible, selective, and orally bioavailable inhibitor of the Akt kinases
Chemical name
N-((S)-1-amino-3-(3-fluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide hydrochloride
Parent CAS No.
[1047644-62-1]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| WDR5-0103 | Axon 2411
CAS [890190-22-4]
MF C21H25N3O4MW 383.44
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Inhibitor of WD40 repeat protein 5 (WDR5) and associated activity of H3K4 HMTase MLL (Kd value 0.45 µM for WDR5 binding, and IC50 value of 39 μM for inhibition of methyltransferase activity of MLL complex). Potential therapeutic for treatment of MLL-rearranged leukemias or other cancers.
References
Certificates
Categories
Extra info
G. Senisterra et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem J. 2013 Jan 1;449(1):151-9.
Y. Bolshan et al. Synthesis, Optimization, and Evaluation of Novel Small Molecules as Antagonists of WDR5-MLL Interaction. ACS Med Chem Lett. 2013 Feb 4;4(3):353-7.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
WDR5
Inhibitor of WD40 repeat protein 5 (WDR5) and associated activity of H3K4 HMTase MLL
Chemical name
methyl 3-(3-methoxybenzamido)-4-(4-methylpiperazin-1-yl)benzoate
Parent CAS No.
[890190-22-4]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| UNC 0379 | Axon 2418
CAS [1620401-82-2]
MF C23H35N5O2MW 413.56
Purity:
98%
Soluble in DMSO
Description
Substrate competitive inhibitor of the H4K20 HMTase SETD8 (IC50 value 7.3 µM) with selectivity over 15 other methyltransferases including G9a and GLP. MOA studies revealed that UNC0379 is noncompetitive with the cofactor S-adenosyl-Lmethionine (SAM).
References
Certificates
Categories
Extra info
A. Ma et al. Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33.
J. Min et al. L3MBTL1 recognition of mono- and dimethylated histones. Nat Struct Mol Biol. 2007 Dec;14(12):1229-30.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
p53-Tumor Suppression
DNA-damage Response
EC 2.1.1.43
HMTase
Substrate competitive inhibitor of the H4K20 HMTase SETD8
Chemical name
6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine
Parent CAS No.
[1620401-82-2]
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Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| SGC2085 | Axon 2625
CAS [1821908-49-9]
MF C19H24N2O2.HClMW 348.87
Purity:
100%
Soluble in water and DMSO
Description
Potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1 or PRMT4) inhibitor (IC50 value 50 nM and >100-fold selectivity over other PRMTs). Unfortunately, no cellular activity was observed for SGC2085 when tested up to 10 μM due to due to poor cell permeability (in HEK293 cells).
KEYWORDS: SGC2085 | supplier | CARM1 inhibitor | SGC-2085 | CAS [1821908-49-9] | [1821908-48-8] | Arginine | PRMT4 | Coactivator Associated Arginine Methyltransferase 1 | oncology | Wnt | β-Catenin | | axonmedchem |
| SGI 1027 dihydrochloride - S 1027 dihydrochloride | Axon 2347
CAS [N.A.]
MF C27H25Cl2N7OMW 534.44
Purity:
99%
Soluble in DMSO
Description
SGI 1027 inhibits DNMT activity (IC50 values 35 μM and 10 μM for DNMT1 and DNMT3A2/3L, respectively) in colon cancer cell lines, and was shown to degrade the enzymes. Prolonged treatment of RKO cells with SGI 1027 led to demethylation and reexpression of the silenced tumor suppressor genes (TSGs) P16, MLH1, and TIMP3 and did not exhibit significant toxicity in a rat hepatoma (H4IIE) cell line. SGI 1027 shows moderate affinity (IC 50 value 65 μM) for G9a-like protein (GLP), another AdoMet-dependent enzyme, as well.
References
Certificates
Categories
Extra info
J. Datta et al.A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation. Cancer Res. 2009, 69, 4277-4285.
S. Valente et al. Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells. J. Med. Chem. 2014, 57, 701-713.
E. Rilova et al. Design, synthesis and biological evaluation of 4-amino-N- (4-aminophenyl)benzamide analogues of quinoline-based SGI-1027 as inhibitors of DNA methylation. ChemMedChem. 2014, 9, 590-601.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
Stem Cell
EC 2.1.1.37
DNA methyltransferase
Inhibitor of DNMT activity in colon cancer cell lines
Chemical name
N-(4-(2-amino-6-methylpyrimidin-4-ylamino)phenyl)-4-(quinolin-4-ylamino)benzamide dihydrochloride
Parent CAS No.
[1020149-73-8]
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Size
Unit Price
Stock
10 mg
€110.00
In Stock | | axonmedchem |
| A-196 | Axon 2705
CAS [1982372-88-2]
MF C18H16Cl2N4MW 359.25
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 ((IC50 values of 25 and 144 nM, respectively). In cells, A-196 induced a global decrease in H4K20me2 and H4K20me3 and a concomitant increase in H4K20me1. A-196 inhibited 53BP1 foci formation upon ionizing radiation and reduced NHEJ-mediated DNA-break repair but did not affect homology-directed repair.
KEYWORDS: A-196 | supplier | SUV4-20 inhibitor | A196 | A 196 | CAS [1982372-88-2] | Non Selective (Lysine Sites Proteins) | PKMT | Inhibitor | Enzymes | Protein Lysine Methyltransferase | Histone Methyltransferase | SUV420H1 | SUV420H2 | | axonmedchem |
| AMI-1 - AMI-1 sodium salt | Axon 2863
CAS [20324-87-2]
MF C21H14N2Na2O9S2MW 548.45
Purity:
99%
Soluble in water and DMSO
Description
AMI-1 specifically inhibits protein arginine N-methyltransferase (PRMT) activity in vitro (IC50 values of 8.81 and 3.04 µM for PRMT1 and Hmt1p, respectively). Furthermore, AMI-1 prevents in vivo arginine methylation of cellular proteins and can modulate nuclear receptor-regulated transcription from estrogen and androgen response elements, thus operating as a brake on certain hormone actions. HIV-1 integrase inhibitor (IC50 value of 4 µM).
KEYWORDS: AMI-1 | supplier | PRMT inhibitor | AMI-1 sodium salt | AMI 1 | AMI1 | CAS [20324-87-2] | [134-47-4] | Non Selective (Arginine Sites Proteins) | PRMT | Inhibitor | Enzymes | HIV-1 | Integrase | Protein Arginine N-Methyltransferase | | axonmedchem |
| EPZ 015666 - GSK 3235025 | Axon 2831
CAS [1616391-65-1]
MF C20H25N5O3MW 383.44
Purity:
99%
Optical purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
EPZ 015666 (GSK 3235025) is a potent, selective and orally available inhibitor of PRMT5 (IC50 value of 22 nM). EPZ 015666 exhibits antiproliferative effects in both in vitro and in vivo models of MCL.
KEYWORDS: EPZ015666 | supplier | PRMT5 inhibitor | GSK3235025 | EPZ-015666 | EPZ 015666 | GSK-3235025 | GSK 3235025 | CAS [1616391-65-1] | Non Selective (Arginine Sites Proteins) | PRMT | Inhibitor | Enzymes | | axonmedchem |
| FMK - RSK inhibitor Fmk | Axon 1848
CAS [821794-92-7]
MF C18H19FN4O2MW 342.37
Purity:
99%
Soluble in DMSO
Description
Potent, highly specific and irreversible inhibitor of p90 ribosomal protein S6 kinase RSK1 and RSK2; FMK binds in the CTKD ATP-binding site and inhibits RSK autophosphorylation at Ser386. FMK induces significant apoptosis in human FGFR3-expressing, t(4;14)-positive multiple myeloma cells.* FMK (IC50 value 15 nM for RSK2 in vitro) is more potent than another CTKD RSK inhibitor SL-0101 (IC50 value 85 nM for RSK2); while BI-D1870 (Axon 1528) binds at NTKD binding site as a reversible RSK inhibitor.
References
Certificates
Categories
Extra info
MS Cohen et al. Structural bioinformatics-based design of selective, irreversible kinase inhibitors. Science 2005, 308(5726),1318–1321.
S Kang et al. p90 ribosomal S6 kinase 2 promotes invasion and metastasis of human head and neck squamous cell carcinoma cells. J. Clin. Invest. 2010, 120(4), 1165–1177.
Doehn et al. RSK Is a Principal Effector of the RAS-ERK Pathway for Eliciting a Coordinate Promotile/Invasive Gene Program and Phenotype in Epithelial Cells. Mol. Cell, 2009, 35(4), 511–522.
TL Nguyen. Targeting RSK: an overview of small molecule inhibitors. Anticancer Agents Med. Chem. 2008, 8(7), 710-716.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MAPK
PI3K-Akt-mTOR
EC 2.7.11.1
p90-RSK
RSK inhibitor (p90 RSK specific)
Chemical name
1-(4-amino-7-(3-hydroxypropyl)-5-p-tolyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl)-2-fluoroethanone
Parent CAS No.
[821794-92-7]
Order
Size
Unit Price
Stock
1 mg
€75.00
In Stock | | axonmedchem |
| CMP5 | Axon 2709
CAS [1030021-40-9]
MF C20H22N3.HClMW 351.87
Purity:
99%
Soluble in water and DMSO
Description
CMP5 is a selective PRMT5 inhibitor that blocked EBV-driven B-lymphocyte transformation and survival while leaving normal B cells unaffected. Also CMP5 inhibited Th1 cell proliferation (IC50 value 3.7 μM) more potently than Th2 cell proliferation (IC50 value 9.2 μM). In vivo, PRMT5 blockade efficiently suppressed recall T cell responses and reduced inflammation in delayed-type hypersensitivity and clinical disease in experimental autoimmune encephalomyelitis mouse models.
Also the more potent and bioavailable derivative HLCL65 hydrochloride is available (Axon 2710). | | axonmedchem |
| EPZ 6438 - Tazemetostat | Axon 2227
CAS [1403254-99-8]
MF C34H44N4O4MW 572.74
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent, selective, and orally bioavailable inhibitor of EZH2 enzymatic activity (IC50 values 2-38 nM in EZH2 assays). Induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells, and dose-dependently leads to regression of malignant rhabdoid tumors (MRTs) with correlative diminution of intratumoral trimethylation levels of H3K27, and prevention of tumor regrowth after dosing cessation.
References
Certificates
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Extra info
S.K. Knutson et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Proc. Natl. Acad. Sci. USA. 2013, 110, 7922-7927.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.1.1.43
Stem Cell Differentiator
HMTase
Inhibitor of Histone Lysine Methyltransferase EZH2
Chemical name
N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)biphenyl-3-carboxamide
Parent CAS No.
[1403254-99-8]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| Axon Ligands™ Epigenetic compound library | Axon 5052
CAS [N.A.]
MF #N/AMW #N/A
Purity:
98%
10 mM in DMSO
Description
Axon Ligands™ Epigenetic compound library. A unique collection of 125 compounds in 96-well microtitter plate (each sample pre-dissolved in DMSO, 250 μL, 10 mM). Our contineously expanding list of compounds for epigenetic research can be found online. They are among most featured and high-profile compounds for epigenetic research.
Cherry-picking! | | axonmedchem |
| Lomeguatrib - PaTrin 2 | Axon 2223
CAS [192441-08-0]
MF C10H8BrN5OSMW 326.17
Purity:
99%
Soluble in DMSO
Description
Potent, orally active inhibitor of O6-methylguanine-DNA-methyltransferase (MGMT; IC50 value 5 nM). Lomeguatrib effectively inactivated MGMT in MCF-7 cells and in xenografts there was complete inactivation of MGMT within 2 h of dosing (20 mg/kg i.p.) and only slight recovery by 24 h.Oral administration of Lomeguatrib substantially increases the haematological toxicity of Dacarbazine, the only approved chemotherapeutic agent for the treatment of metastatic melanoma. In combination with Temozolomide, Lomeguatrib produced a substantial tumour growth delay in MCF-7 xenografts.
References
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Extra info
H.A. Tawbi et al. Inhibition of DNA repair with MGMT pseudosubstrates: phase I study of lomeguatrib in combination with dacarbazine in patients with advanced melanoma and other solid tumours. Br. J. Cancer. 2011, 105, 773-777.
M. Clemons et al. O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumour MCF-7 cells and xenografts. Br. J. Cancer. 2005, 93, 1152-1156.
M. Turriziani et al. O6-(4-bromothenyl)guanine (PaTrin-2), a novel inhibitor of O6-alkylguanine DNA alkyl-transferase, increases the inhibitory activity of temozolomide against human acute leukaemia cells in vitro. Pharmacol. Res. 2006, 53, 317-323.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
Stem Cell
EC 2.1.1.63
DNA methyltransferase
Potent, orally active inhibitor of MGMT
Chemical name
6-((4-bromothiophen-2-yl)methoxy)-7H-purin-2-amine
Parent CAS No.
[192441-08-0]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| Axon Ligands™ Stem cell compound library | Axon 5053
CAS [N.A.]
MF #N/AMW #N/A
Purity:
98%
10 mM in DMSO
Description
Axon Ligands™ Stem cell compound library: A unique collection of >140 compounds for stem cell research in 96-well microtitter plate (each sample pre-dissolved in DMSO, 250 μL, 10 mM). Our contineously expanding list of compounds for stem cell research can be found online. They are among most featured and high-profile compounds for stem cell research.
Cherry-picking! | | axonmedchem |
| WAY-267464 dihydrochloride | Axon 2711
CAS [1432043-31-6]
MF C32H35N7O4.2HClMW 654.59
Purity:
98%
Soluble in water and DMSO
Description
WAY-267464 is a non-peptide high-affinity, potent, and selective agonist of the oxytocin receptor (Ki value of 58.4 nM at human OTR).
KEYWORDS: WAY-267464 dihydrochloride | supplier | OTR agonist | WAY 267,464 dihydrochloride | CAS [1432043-31-6] | [847375-16-0] | Oxytocin | Agonist | Receptors | OTR | WAY-267464 | | axonmedchem |
| HLCL65 hydrochloride | Axon 2710
CAS [N.A.]
MF C23H23BrN2O.HClMW 459.81
Purity:
99%
Soluble in DMSO
Description
HLCL65 is a highly selective small molecule PRMT5 inhibitor. HLCL65 inhibited Th1 cell proliferation (IC50 value 1.1 μM) more potently than Th2 cell proliferation (IC50 value 4 μM). In vivo, PRMT5 blockade efficiently suppressed recall T cell responses and reduced inflammation in delayed-type hypersensitivity and clinical disease in experimental autoimmune encephalomyelitis mouse models.
HLCL65 is a more potent and bioavailable derivative of CMP5 (Axon 2709).
KEYWORDS: HLCL65 hydrochloride | supplier | PRMT5 inhibitor | HLCL-65 | HLCL 65 | CAS [1627865-11-5] | Non Selective (Arginine Sites Proteins) | PRMT | Inhibitor | Enzymes | | axonmedchem |
| PRMT3 inhibitor 1 - Compound 1 | Axon 2211
CAS [1340875-03-7]
MF C15H18N4OSMW 302.39
Purity:
99%
Soluble in DMSO
Description
Allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3; IC50 value of 1.6 μM for inhibition of full length PRMT3 in a radioactivity-based assay). PRMT3 inhibitor 1 showed no inhibitory activity on any of the PKMTs G9a, EHMT1, SUV39H2, SETD7, and SETD8, and PRMTs PRMT1, PRMT4, PRMT5, and PRMT8.The allosteric binding site of compound 1 was localized by site-directed mutagenesis of PRMT3 and X-ray crystallography.
References
Certificates
Categories
Extra info
A. Siarheyeva et al. An allosteric inhibitor of protein arginine methyltransferase 3. Structure. 2012, 20, 1425-1435.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
Endocrinology
EC 2.1.1.125
PRMT
Allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3)
Chemical name
1-(benzo[d][1,2,3]thiadiazol-6-yl)-3-(2-cyclohexenylethyl)urea
Parent CAS No.
[1340875-03-7]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| C 7280948 | Axon 2210
CAS [587850-67-7]
MF C14H16N2O2SMW 276.35
Purity:
99%
Soluble in DMSO
Description
Sulfone inhibitor of PRMT1 (IC50 values 12.75 μM and 26.7 μM for oligopeptide that contains the amino acids 1–21 of human histone H4 and non-histone protein Npl3 as methylation substrates respectively). Useful tool in studying the epigenetic role of PRMT1. PRMT1 has been linked to the activation of estrogen and androgen receptors as well. PRMT1 is a necessary component for oncogenic transformation induced by a mixed lineage leukemia (MLL) complex, and therefore may represent a new treatment option for hormone-dependent cancer.
References
Certificates
Categories
Extra info
R. Heinke et al. Virtual Screening and Biological Characterization of Novel Histone Arginine Methyltransferase PRMT1 Inhibitors. ChemMedChem 2009, 4, 69-77.
E.M. Bissinger et al. Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1. Bioorg. Med. Chem. 2011, 19, 3717–3731.
Y Itoh et al. Small-molecular modulators of cancer-associated epigenetic mechanisms. Mol. BioSyst. , 2013, 9, 873-896.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
Endocrinology
EC 2.1.1.125
PRMT
Sulfone inhibitor of PRMT1
Chemical name
4-amino-N-phenethylbenzenesulfonamide
Parent CAS No.
[587850-67-7]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| UNC 0638 | Axon 1889
CAS [1255580-76-7]
MF C30H47N5O2MW 509.73
Purity:
98%
Soluble in DMSO
Description
Potent and selective G9a (EHMT2)/GLP (EHMT1) inhibitor (G9a IC50: <15 nM; GLP IC50: 19 nM); chemical probe for G9a and GLP methyltransferase inhibition in cells
References
Certificates
Categories
Extra info
M Vedadi et al. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat. Chem. Biol. 2011, 7(8), 566-574.
F Liu et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J. Med. Chem. 2011, 54(17), 6139-6150.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.1.1.43
HMTase
Inhibitor of G9a (EHMT2)/GLP (EHMT1)
Chemical name
2-cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine
Parent CAS No.
[1255580-76-7]
Order
Size
Unit Price
Stock
2 mg
€85.00
In Stock | | axonmedchem |
| GSK 126 | Axon 2140
CAS [1346574-57-9]
MF C31H38N6O2MW 526.67
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent, selective, cell-active inhibitor of histone lysine methyltransferase (HMTase or HMT; H3K27 selective) EZH2 (Ki 0.57 nM; IC50 9.9 nM); more than 150-fold selective for EZH2 versus EZH1 (Ki 89 nM) and 20 other human methyltransferases. GSK126 effectively inhibits proliferation of EZH2 mutant DLBCL cell lines and growth of EZH2 mutant DLBCL xenografts in mice.
References
Certificates
Categories
Extra info
MT McCabe et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature. 2012, 492, 108-112.
SK Verma et al. Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med. Chem. Lett. 2012, 3, 1091−1096.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.1.1.43
HMTase
Inhibitor of Histone Lysine Methyltransferase EZH2
Chemical name
(S)-1-sec-butyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide
Parent CAS No.
[1346574-57-9]
Order
Size
Unit Price
Stock
2 mg
€75.00
In Stock | | axonmedchem |
| UNC 0646 | Axon 1840
CAS [1320288-17-2]
MF C36H59N7O2MW 621.90
Purity:
99%
Soluble in DMSO
Description
Very potent and selective G9a/GLP protein lysine methyltransferase inhibitor (G9a IC50: 6 nM; GLP IC50: 15 nM); with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity
References
Certificates
Categories
Extra info
F Liu et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J. Med. Chem. 2011, 54(17), 6139-6150.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.1.1.43
HMTase
Inhibitor of G9a/GLP Histone Lysine Methyltransferase
Chemical name
N-(1-cyclohexylpiperidin-4-yl)-2-(4-isopropyl-1,4-diazepan-1-yl)-6-methoxy-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-amine
Parent CAS No.
[1320288-17-2]
Order
Size
Unit Price
Stock
5 mg
€99.00
In Stock | | axonmedchem |
| Decitabine | Axon 1590
CAS [2353-33-5]
MF C8H12N4O4MW 228.21
Purity:
99%
Soluble in water and DMSO
Description
DNA methyltransferase inhibitor; a therapeutical agent to treat myelodysplastic syndromes (MDS)
References
Certificates
Categories
Extra info
H Kantarjian et al. Decitabine improves patient outcomes in myelodysplastic syndromes: results of a phase III randomized study. Cancer 2006, 106(8), 1794–803.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
Stem Cell
EC 2.1.1.37
DNA methyltransferase
DNA methyltransferase inhibitor
Chemical name
4-amino-1-((2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1,3,5-triazin-2(1H)-one
Parent CAS No.
[2353-33-5]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| Zebularine | Axon 1254
CAS [3690-10-6]
MF C9H12N2O5MW 228.20
Purity:
99%
Soluble in water
Description
DNA methyltransferase inhibitor, aka DNA methylation inhibitor, anticancer drug
References
Certificates
Categories
Extra info
L Zhou et al. Zebularine: a novel DNA methylation inhibitor that forms a covalent complex with DNA methyltransferases. J. Mol. Biol. 2002, 321(4), 591-599.
Yoo, C.B. et al. Zebularine: a new drug for epigenetic therapy. Biochem Soc Trans. 2004, 32, 910-912.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
Stem Cell
EC 2.1.1.37
Stem Cell Differentiator
DNA methyltransferase
DNA methyltransferase inhibitor
Chemical name
1-((2R,3R,4S,5R)-3,4-Dihydroxy-5-hydroxymethyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one
Parent CAS No.
[3690-10-6]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| RG 108 | Axon 1691
CAS [48208-26-0]
MF C19H14N2O4MW 334.33
Purity:
99%
Optical purity:
>98% ee
Soluble in DMSO
Description
DNA methyltransferase inhibitor; Inhibits DNA methylation in human cancer cell lines in vitro without detectable toxicity; Demethylates and reactivates epigenetically silenced tumor suppressor genes. Recently, BIX01294 (Axon 1692) and RG108 have been reported to enhance the efficiency of induced pluripotent stem cell (iPS) generation
*Promotion | | axonmedchem |
| UNC 0631 | Axon 1841
CAS [1320288-19-4]
MF C37H61N7O2MW 635.93
Purity:
98%
Soluble in DMSO
Description
Very potent and selective G9a/GLP protein lysine methyltransferase inhibitor (G9a IC50: 6 nM; GLP IC50: 15 nM); with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity
References
Certificates
Categories
Extra info
F Liu et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J. Med. Chem. 2011, 54(17), 6139-6150.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.1.1.43
HMTase
Inhibitor of G9a/GLP Histone Lysine Methyltransferase
Chemical name
N-(1-(cyclohexylmethyl)piperidin-4-yl)-2-(4-isopropyl-1,4-diazepan-1-yl)-6-methoxy-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-amine
Parent CAS No.
[1320288-19-4]
Order
Size
Unit Price
Stock
5 mg
€99.00
In Stock | | axonmedchem |
| BI-D1870 | Axon 1528
CAS [501437-28-1]
MF C19H23F2N5O2MW 391.42
Purity:
99%
Soluble in DMSO and Ethanol
Description
Potent and specific inhibitor of the p90 ribosomal S6 kinase (RSK) isoforms in vitro and in vivo, which inhibits RSK1, RSK2, RSK3 and RSK4 in vitro (IC50 values 31 nM, 24 nM, 18 nM, and 15 nM, respectively).* BI-D1870 binds at NTKD binding site as a reversible RSK inhibitor, while FMK (Axon 1848) binds at CTKD site as an irreversible RSK inhibitor.
KEYWORDS: BI-D1870 | supplier | RSK inhibitor | BID1870 | BID-1870 | CAS [501437-28-1] | p90-RSK | p90 ribosomal S6 kinase | RSK1 | RSK2 | RSK3 | RSK4 | NTKD binding site | reversible | | axonmedchem |
| ABT 239 tartrate | Axon 1510
CAS [ 460748-71-4]
MF C22H22N2O.C4H6O6MW 480.51
Purity:
98%
Optical purity:
>98% ee
Soluble in water and DMSO
Description
Potent and selective histamine H3 receptor antagonist or inverse agonist; a highly recommended tool for animal research into H3 antagonist / inverse agonist
References
Certificates
Categories
Extra info
TA Esbenshade et al. Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties. J. Ph. Exp. Ther. 2005, 313, 165.
GB Fox et al. Pharmacological properties of ABT-239 : II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist. J. Ph. Exp. Ther. 2005, 313, 176–90.
M Cowart et al. 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. J. Med. Chem. 2005, 48 (1), 38–55.
Certificate of Analysis
Material Safety Data Sheet
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
H3
A18
H3 antagonist/inverse agonist
Chemical name
4-{2-[2-((R)-2-Methyl-pyrrolidin-1-yl)-ethyl]-benzofuran-5-yl}-benzonitrile tartrate
Parent CAS No.
[460746-46-7]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| A 943931 | Axon 1990
CAS [1027330-97-7]
MF C17H21N5MW 295.38
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and selective histamine H4 receptor antagonist
References
Certificates
Categories
Extra info
MD Cowart et al. Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. J. Med. Chem. 2008, 51, 6547.
R Leurs et al. Molecular and biochemical pharmacology of the histamine H4 receptor. Br. J. Pharmacol. 2009, 157, 14.
RA Smits et al. Major advances in the development of histamine H4 receptor ligands. Drug Disc. Today. 2009, 14(15-16), 745.
Certificate of Analysis
Material Safety Data Sheet
CNS
Immunology
H4
A18
H4 antagonist
Chemical name
4-[(3R)-3-aminopyrrolidin-1-yl]-6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-d]pyrimidin-2-amine
Parent CAS No.
[1027330-97-7]
Order
Size
Unit Price
Stock
2 mg
€75.00
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