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Chemical Structure : GSK3484862
CAS No.: 2170136-65-7
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $188 | In stock | |
| 25 mg | $298 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 365.455 | |
| Formula | C19H19N5OS | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(R)-2-((3,5-dicyano-6-(dimethylamino)-4-ethylpyridin-2-yl)thio)-2-phenylacetamide |
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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.
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