GSK3484862 (GSK-3484862)

Chemical Structure : GSK3484862

CAS No.: 2170136-65-7

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货号: PC-72245Not For Human Use, Lab Use Only.

GSK3484862 (GSK-3484862) is a selective, non-covalent inhibitor of DNMT1, potently inhibits DNMT1 enzymatic activity with IC50 of 0.23 uM.

规格	价格	库存
5 mg	￥1380	In stock
10 mg	￥2180	In stock
25 mg	￥3880	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

GSK3484862 (GSK-3484862) is a selective, non-covalent inhibitor of DNMT1, potently inhibits DNMT1 enzymatic activity with IC50 of 0.23 uM.
GSK3484862 showed no inhibition of the family members DNMT3A/3L and DNMT3B/3L, or the assay coupling enzyme Gla1 at 50 uM.
GSK3484862 is chemically stable, did not bind DNA nonspecifically, and resulted in rapidly reversible inhibition of DNMT1.
GSK-3484862 mediates striking demethylation in murine embryonic stem cells (mESCs) with minimal non-specific toxicity.
Cellular engagement of DNMT1 by GSK3484862 resulted in a dose-dependent loss of promoter DNA methylation and marked transcriptional up-regulation of vimentin in HCT-116 cells.
GSK3484862 reprogrammed mouse embryonic fibroblast C3H/10T1/2 cells into functional muscle or fat cells by expression of the Myod1 or Adipoq differentiation marker genes.

物理化学性质&存储条件

分子量	365.455
分子式	C19H19N5OS
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	(R)-2-((3,5-dicyano-6-(dimethylamino)-4-ethylpyridin-2-yl)thio)-2-phenylacetamide

参考文献

1. Nathalia Azevedo Portilho, et al. Epigenetics Chromatin. 2021 Dec 15;14(1):56.

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