Catalog No.: 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).
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.
