SKLB-03176
Modify Date: 2024-04-08 12:40:20
SKLB-03176 structure
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Common Name | SKLB-03176 | ||
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| CAS Number | 2609675-22-9 | Molecular Weight | 514.63 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C29H34N6O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of SKLB-03176SKLB-03176 (SKLB03176) is a potent, selective, covalent EZH2 inhibitor with IC50 of 47 nM, covalently binds to the SAM pocket of EZH2.SKLB-03176 showed good inhibitory activity against mutations EZH2 Y641F, EZH2 Y641N, and EZH2A677G at 200 nM concentration.SKLB-03176 exhibited weak activity against other targets, such as 5 histone methyltransferases and more than 30 kinases, >50-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 (IC50=2.45 uM).SKLB-03176 inhibited the activity of a variety of EZH2 mutants and significantly inhibited the expression of H3K27Me3 in cells.SKLB-03176 showed no cytotoxicity to normal cells. |
| Name | SKLB-03176 |
|---|
| Description | SKLB-03176 (SKLB03176) is a potent, selective, covalent EZH2 inhibitor with IC50 of 47 nM, covalently binds to the SAM pocket of EZH2.SKLB-03176 showed good inhibitory activity against mutations EZH2 Y641F, EZH2 Y641N, and EZH2A677G at 200 nM concentration.SKLB-03176 exhibited weak activity against other targets, such as 5 histone methyltransferases and more than 30 kinases, >50-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 (IC50=2.45 uM).SKLB-03176 inhibited the activity of a variety of EZH2 mutants and significantly inhibited the expression of H3K27Me3 in cells.SKLB-03176 showed no cytotoxicity to normal cells. |
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| References | 1. Zhang Q, et al. Biomed Pharmacother. 2022 Mar;147:112617. |
| Molecular Formula | C29H34N6O3 |
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| Molecular Weight | 514.63 |