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GSK3685032 is a potent first-in-class DNMT1-selective inhibitor. 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.
| Molecular Weight | 420.53 |
| Formula | C22H24N6OS |
| CAS Number | 2170137-61-6 |
| Solubility (25°C) | DMSO >20mg/ml |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related DNA Methyltransferase Products |
|---|
| Decitabine
Decitabine (5-Aza-2'-deoxycytidine) is a potent inhibitor of DNA methylation for the treatment of myelodysplastic syndromes. |
| RG108
RG108 is a novel small-molecule inhibitors of DNA methyltransferases with IC50 of 115 nM. |
| Lomeguatrib
Lomeguatrib is a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase with IC50 of 5 nM. |
| SGI-1027
SGI-1027 is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B |
| SGI-110
SGI-110 (S-110) is a stable and potent inhibitor for DNA methylation, inhibits DNMT1 when SGI-110 is activated by phosphorylation and incorporated into DNA. |
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