1. Epigenetics
  2. Histone Methyltransferase
  3. MRK-740

MRK-740 

目录号: HY-114209
产品使用指南

MRK-740 是一种有效的,选择性的,与底物竞争的 PRDM9 组蛋白甲基转移酶抑制剂,IC50 为 80 nM。MRK-740 对 PRDM9 的选择性高于其他组蛋白甲基转移酶和其他非表观遗传靶标。MRK-740 减少 PRDM9 依赖性的 H3K4 三甲基化 (IC50 为 0.8 µM)。

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MRK-740 Chemical Structure

MRK-740 Chemical Structure

CAS No. : 2387510-80-5

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Description

MRK-740 is a potent, selective and substrate-competitive PRDM9 histone methyltransferase inhibitor with an IC50 of 80 nM. MRK-740 is more selective for PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 reduces PRDM9-dependent trimethylation of H3K4 (IC50 = 0.8 µM)[1].

IC50 & Target

IC50: 80 nM (PRDM9)[1]

In Vitro

After 24 h of treatment, MRK-740 (3 µM) does not affect HEK293T cell growth at the IC90, but some toxicity is observed at 10 µM. MRK-740 is an equipotent inhibitor of H3K4 methylation in MCF7 cells. In cells, MRK-740 specifically and directly inhibits H3K4 methylation at endogenous PRDM9 target loci[1].

Molecular Weight

464.56

Formula

C₂₅H₃₂N₆O₃

CAS No.

2387510-80-5

SMILES

CC1=NC=CC(N(CC2)CCC32CN(C4=NC(C5=CC(OC)=CC(OC)=C5)=NO4)CCN3C)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

MRK-740MRK740MRK 740Histone MethyltransferasePRDM9substrate-competitiveH3K4trimethylationInhibitorinhibitorinhibit

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产品名称:
MRK-740
目录号:
HY-114209
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