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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-MS8535
MS8535

Chemical Structure : MS8535

CAS No.:

MS8535 (MS-8535, MS 8535)

货号: PC-22053Not For Human Use, Lab Use Only.

MS8535 is a potent, selective and cell-active inhibitor of methyl-lysine reader protein SPIN1 with biochemical IC50 of 202 nM and ITC binding Kd of 30 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MS8535 is a potent, selective and cell-active inhibitor of methyl-lysine reader protein SPIN1 with biochemical IC50 of 202 nM and ITC binding Kd of 30 nM.
MS8535 displays high selectivity for SPIN1 over 38 epigenetic targets, including G9a/GLP, and >18-fold selective for SPIN1 over several other SPIN family members, such as SPIN2B (Kd = 0.56 μM), SPIN3 (Kd = 1.4 μM), and SPIN4 (Kd = 0.71 μM).
MS8535 concentration dependently blocks the interactions between SPIN1 and histone H3 in U2OS cells with EC50 of 1.1 uM in NanoBRET assay.

物理化学性质&存储条件

分子量 490.65
分子式 C28H38N6O2
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

N1-(7-(3-(Isoindolin-2-yl)propoxy)-6-methoxy-4-(pyrrolidin-1-yl)quinazolin-2-yl)-N2,N2-dimethylethane-1,2-diamine

参考文献

1. Yan Xiong, et al. J Med Chem. 2024 Mar 27. doi: 10.1021/acs.jmedchem.4c00121.

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