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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-MRK-740
MRK-740

Chemical Structure : MRK-740

CAS No.: 2387510-80-5

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MRK-740 (MRK740)

货号: PC-73122Not For Human Use, Lab Use Only.

MRK-740 (MRK740) is a first-in-class, potent, selective and cell-active PRDM9 inhibitor with IC50 of 80 nM.

规格 价格 库存 数量
5 mg ￥980 In stock
10 mg ￥1480 In stock
25 mg ￥2580 In stock
50 mg ￥4280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MRK-740 (MRK740) is a first-in-class, potent, selective and cell-active PRDM9 inhibitor with IC50 of 80 nM.
MRK-740 is much less potent at inhibiting PRDM7 (IC50=45 uM), doest not inhibits 11 other PRDM family members, also shows selectivity against a panel of 108 enzymes and receptors.
MRK-740 binds in the substrate-binding pocket (SPR Kd=87 nM), with unusually extensive interactions with the cofactor SAM, conferring SAM-dependent substrate-competitive inhibition.
MRK-740 engages PRMD9 and inhibits PRDM9-dependent trimethylation of ectopic H3K4 (EC50=0.8 uM) and endogenous H3K4 in in HEK293T cells, with minimal impact on cell viability.
MRK-740 specifically inhibits PRDM9-dependent methylation on endogenous chromatin, but does not affect H3K4 methylation activity from non-PRDM9 sources.
MRK-740 does not affect proliferation of cancer cell lines.
MRK-740 is a chemical probe for the PRDM subfamily of methyltransferases.

物理化学性质&存储条件

分子量 464.57
分子式 C25H32N6O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-(3,5-Dimethoxyphenyl)-5-(1-methyl-9-(2-methylpyridin-4-yl)-1,4,9-triazaspiro[5.5]undecan-4-yl)-1,2,4-oxadiazole

参考文献

1. Allali-Hassani A, et al. Nat Commun. 2019 Dec 17;10(1):5759.

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