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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-AS-254s
AS-254s

Chemical Structure : AS-254s

CAS No.:

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AS-254s (Compound 66s, AS254s)

货号: PC-23618Not For Human Use, Lab Use Only.

AS-254s is a highly potent and selective histone lysine methyltransferase ASH1L (absent, small, or homeotic-like 1) inhibitor with IC50 of 94 nM in FP assays, binds to the catalytic SET domain of ASH1L with ITC Kd of 179 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AS-254s is a highly potent and selective histone lysine methyltransferase ASH1L (absent, small, or homeotic-like 1) inhibitor with IC50 of 94 nM in FP assays, binds to the catalytic SET domain of ASH1L with ITC Kd of 179 nM.
AS-254s exhibits pronounced ASH1L inhibition (IC50=0.15 μM in HMT assay).
AS-254s shows no inhibitory activity against a panel of 15 other histone methyltransferases, including closely related NSD family of HMTs.
AS-254s markedly reduces the H3K36me2 level in a dose-dependent manner in ASH1L-dependent leukemic MV4;11 cells (harboring MLL-AF4 translocation) and KOPN8 cells (harboring MLL-ENL translocation), with no effect on the global level of H3.
AS-254s demonstrates time-dependent cell growth inhibition in the ASH1L-dependent MV4;11 leukemia cells with GI50 values from 6.8 to 0.74 μM between day 3 and day 14 of treatment.
AS-254s (1-5 uM) induces apoptosis differentiation of MLL1-r leukemia MV4;11 and KOPN8 cells.
AS-254s could strongly recapitulate the effects observed upon genetic inactivation of ASH1L or deletion of the SET domain in the MLL1-rearranged leukemia cells.

物理化学性质&存储条件

分子量 741.79
分子式 C36H42Cl2N6O3S2
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

N-(2-(2-(((3-(3-carbamothioylphenyl)-7-chloro-1-(tetrahydro-2H-pyran-4-yl)-1H-indol-6-yl)methyl)carbamoyl)-7-azaspiro[3.5]nonan-7-yl)ethyl)thiazole-2-carboxamide hydrochloride

参考文献

1. Huang G, et al. J Med Chem. 2024 Dec 16. doi: 10.1021/acs.jmedchem.4c01673.

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