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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 |
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| Benzyl selenocyanate
Benzyl selenocyanate is a chemopreventive agent for various chemically induced tumors in animal models at both the initiation and postinitiation stages. |
| (S)-GSK-3685032
(S)-GSK-3685032 is the inactive isomer of GSK-3685032.GSK-3685032 is a non-time-dependent, non-covalent, first-in-class, reversible selective inhibitor of DNMT1 with an IC50 value of 0.036 μM.GSK-3685032 induces DNA GSK-3685032 induces loss of DNA methylation, transcriptional activation and cancer cell growth inhibition. |
| (R)-GSK-3685032
(R)-GSK-3685032 is the R-isomer of GSK-3685032.GSK-3685032 is a non-time-dependent, non-covalent, first-in-class, reversible selective inhibitor of DNMT1 with an IC50 value of 0.036 μM.GSK-3685032 induces DNA GSK-3685032 induces loss of DNA methylation, transcriptional activation and cancer cell growth inhibition. |
| DNMT-IN-1
DNMT-IN-1 is a potent DNMT inhibitor with an EC50 value of 3.2 µM. |
| DNMT2-IN-1
DNMT2-IN-1 is a potent and selective DNMT2 (DNA methyltransferase 2) inhibitor with an IC50 value of 1.2 μM, and has the potential for mental and metabolic disorders or cancer research. |
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