| CAS NO: | 2237942-08-2 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Cas No. | 2237942-08-2 |
| 别名 | (rel)-MC180295 |
| Canonical SMILES | NC1=C(C(C2=CC=CC=C2[N+]([O-])=O)=O)SC(N[C@@H]3[C@H](C4)CC[C@H]4C3)=N1 |
| 分子式 | C17H18N4O3S |
| 分子量 | 358.41 |
| 溶解度 | DMSO : 100 mg/mL (279.01 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | (rel)-MC180295 is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. (rel)-MC180295 also inhibits GSK-3α and GSK-3β. (rel)-MC180295 has potent anti-tumor effect[1]. (rel)-MC180295 (MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs, such as CDK1-Cyclin B (IC50, 138 nM), CDK2-Cyclin A (IC50, 233 nM), CDK2-Cyclin E (IC50, 367 nM), CDK3-Cyclin E (IC50, 399 nM), CDK4-Cyclin D (IC50, 112 nM), CDK5-P35 (IC50, 159 nM), CDK5-P25 (IC50, 186 nM), CDK6-Cyclin D3 (IC50, 712 nM), and CDK7-CycH/MAT1 (IC50, 555 nM). (rel)-MC180295 also inhibits GSK-3α and GSK-3β[1].(rel)-MC180295 (500 nM) reactivates epigenetically silenced genes by targeting CDK9 without affecting DNA methylation[1].(rel)-MC180295 (0.1 μM) inhibits the proliferation in cancer cells[1]. (rel)-MC180295 (MC180295; 20 mg/kg, i.p., qod) inhibits significant anti-tumor activity in mice bearing SW48 cells, shows no inhibitory activity against human T cell growth in vivo[1]. [1]. Zhang H, et al. Targeting CDK9 Reactivates Epigenetically Silenced Genes in Cancer. Cell. 2018 Nov 15;175(5):1244-1258.e26. |
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