S83036 |
BRD9539 |
源葉(MedMol) | 98% |
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- 產(chǎn)品描述: BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1
- 靶點: G9a:6.3 μM (IC50);PRC2;HistoneMethyltransferase
- 體外研究:
BRD9539 decreases ATP levels in a dose-dependent manner in HeLa cells.
BRD9539 is a more potent biochemical inhibitor than its methyl-ester analogue BRD4770, with 20% remaining G9a activity compared to 45% of BRD4770 at screening concentration. However, BRD9539 has no activity in cell-based assays, presumably due to impaired cell permeability compared to that of BRD4770. In addition, the activities of 16 other chromatin-modifying enzymes and 100 kinases involved in cell-cycle regulation and cancer cell biology are tested for activity in the presence of 5 or 10 μM BRD9539; no activity is seen in any of these assays.
- 參考文獻(xiàn):
1. Yuan, Y., Wang, Q., Paulk, J., et al. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma ACS Chem. Biol. 7(7), 1152-1157 (2012).
- 溶解性: Soluble in DMSO
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 2.503 ml 12.517 ml 25.035 ml 5 mM 0.501 ml 2.503 ml 5.007 ml 10 mM 0.25 ml 1.252 ml 2.503 ml 50 mM 0.05 ml 0.25 ml 0.501 ml
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