GSK3482364 | DNMT1 inhibitor | Probechem Biochemicals

Chemical Structure : GSK3482364

CAS No.: 2170136-02-2

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GSK3482364 ((Rac)-GSK-3484862)

货号: PC-26177Not For Human Use, Lab Use Only.

GSK3482364 (GSK348236428) is a selective, reversible, orally active inhibitor of DNMT1 with IC50 of 0.4 uM, >375-fold selectivity over DNMT3A/3L and DNMT3B/3L (IC50>150 uM).

规格	价格	库存
5 mg	￥1180	In stock
10 mg	￥1880	In stock
25 mg	￥3280	In stock
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100 mg		Get quote

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生物&药学活性

GSK3482364 (GSK34823642) is a selective, reversible, orally active inhibitor of DNMT1 with IC50 of 0.4 uM, >375-fold selectivity over DNMT3A/3L and DNMT3B/3L (IC50>150 uM).
GSK3482364 reduced 5-methylcytosine levels in a dose-dependent manner with IC50 of 0.24 uM in erythroid progenitor cells (EPCs), decreased methylation of the -53 bp HBG1/ HBG2 cytosine residues with IC50 of 0.33 uM.
GSK3482364 does not require DNA incorporation and is reversible, in contrast with cytidine analog DNMT inhibitor decitabine.
GSK3482364 (100 mg/kg, b.i.d. p.o.) caused significant increases in both HbF levels and in the percentage HbF-expressing erythrocytes in a transgenic mouse model of sickle cell disease.

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	2-((3,5-dicyano-6-(dimethylamino)-4-ethylpyridin-2-yl)thio)-2-phenylacetamide

参考文献

1. Aidan G Gilmartin, et al. Haematologica. 2021 Jul 1;106(7):1979-1987.

GSK3482364 ((Rac)-GSK-3484862)

生物&药学活性

物理化学性质&存储条件

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GSK3482364 ((Rac)-GSK-3484862)

生物&药学活性

物理化学性质&存储条件

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