GSK3685032 (GSK-3685032)

Chemical Structure : GSK3685032

CAS No.: 2170137-61-6

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货号: PC-72244Not For Human Use, Lab Use Only.

GSK3685032 (GSK-3685032) is a potent, first-in-class, highly selective DNMT1 inhibitor with IC50 of 36 nM, >2,500-fold over DNMT3A/3L and DNMT3B/3L.

规格	价格	库存
5 mg	￥1480	In stock
10 mg	￥2180	In stock
25 mg	￥3880	In stock
50 mg	￥5980	In stock
100 mg		Get quote

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生物&药学活性

GSK3685032 (GSK-3685032) is a potent, first-in-class, highly selective DNMT1 inhibitor with IC50 of 36 nM, >2,500-fold over DNMT3A/3L and DNMT3B/3L.
GSK3685032 exhibited IC50 >10 uM against broad panels of other methyltransferases.
GSK3685032 displayed a >350-fold reduction in the inhibition of recombinant H1507Y mutant protein when compared with wild-type DNMT1.
GSK3685032 showed potent anti-proliferative effect in a panel of 51 hematologic cancer cell lines with median growth IC50 (gIC50) of 0.64 uM.
GSK3685032 induces changes in DNA methylation and gene expression in treated cells, activates immune response pathways.
GSK3685032 reveals improved in vivo efficacy and tolerability in AML models compared with decitabine.

物理化学性质&存储条件

分子量	420.535
分子式	C22H24N6OS
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	2-((6-(4-aminopiperidin-1-yl)-3,5-dicyano-4-ethylpyridin-2-yl)thio)-2-phenylacetamide

参考文献

1. Melissa B Pappalardi, et al. Nat Cancer. 2021 Oct;2(10):1002-1017.