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Chemical Structure : SKLB-03220
Catalog No.: PC-49699Not For Human Use, Lab Use Only.
SKLB-03220 (SKLB03220) is a potent, selective EZH2 covalent inhibitor with IC50 of 1.72 nM (EZH2 WT).
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SKLB-03220 (SKLB03220) is a potent, selective EZH2 covalent inhibitor with IC50 of 1.72 nM (EZH2 WT).
SKLB-03220 binds the same location as the EPZ-6438, and forms a covalent bond with Cys663.
SKLB-03220 (10 nM) showed good inhibitory activity against EZH2 mutants (EZH2 A677G, EZH2 Y641N, and EZH2 Y641F).
SKLB-03220 does not exhibit inhibitory activity against other HMTases at 10 uM (G9a, SUV39H1, SETD8, SMYD2, PRMT1, PRMT5, and PRMT7), as well as a panel of 224 kinases by Eurofins Kinase Profiler.
SKLB-03220 exhibited more potent proliferation inhibitory activity than reference compounds GSK126 and EPZ-6438, especially in human ovarian cancer cell lines.
SKLB-03220 inhibited proliferation of ovarian cancer cell lines PA-1 and A2780 with IC50 of 10.1 and 11.2 uM, respectively, induced ovarian cancer cell apoptosis in a dose-dependent manner, inhibited the expression of H3K27me3 in ovarian cancer cells.
SKLB-03220 (150 mg/kg, oral, twice daily) reduced the tumor growth in PA-1 tumor xenograft model in BALB/c nude mice, exhibited greater tumor growth inhibition (TGI) than EPZ-6438 (150 mg/kg) group.
| M.Wt | 556.71 | |
| Formula | C33H40N4O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Qiangsheng Zhang, et al. J Med Chem. 2023 Jan 24. doi: 10.1021/acs.jmedchem.2c01370.
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