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Chemical Structure : GSK3482364
CAS No.: 2170136-65-7
Catalog No.: PC-72246Not 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).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $228 | In stock | |
| 25 mg | $468 | In stock | |
| 100 mg | Get quote |
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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).
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.
| M.Wt | 365.455 | |
| Formula | C19H19N5OS | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO (3.7 mg/mL) |
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| Chemical Name/SMILES |
(αR)-α-[[3,5-Dicyano-6-(dimethylamino)-4-ethyl-2-pyridinyl]thio]benzeneacetamide |
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1. Aidan G Gilmartin, et al. Haematologica. 2021 Jul 1;106(7):1979-1987.
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