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CAS No. | 2170137-61-6 | Cat. No. | BCP43733 |
Related Products | GSK3685032TFA(GSK3685032 TFA ) 2170140-50-6((R)-GSK-3685032) | ||
Name | GSK3685032 | ||
Synonyms | GSK-3685032;GSK 3685032; | ||
SMILES | CCC1=C(C(=NC(=C1C#N)SC(C2=CC=CC=C2)C(=O)N)N3CCC(CC3)N)C#N | ||
Chemical Name | |||
Formula | C22H24N6OS | M. Wt | 420.54 |
Purity | 98% | Storage | Store at 4-8°C |
Description | GSK3685032, a potent first-in-class DNMT1-selective inhibitor that was shown via crystallographic studies to compete with the active-site loop of DNMT1 for penetration into hemi-methylated DNA between two CpG base pairs. GSK3685032 induces robust loss of DNA methylation, transcriptional activation and cancer cell growth inhibition in vitro. Due to improved in vivo tolerability compared with decitabine, GSK3685032 yields superior tumor regression and survival mouse models of acute myeloid leukemia. |
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