(rel)-MC180295 (Synonyms: (rel)-MC180295) |
| Catalog No.GC34124 |
(rel)-MC180295((rel)-(rel)-MC180295)는 IC50이 5nM이고 다른 CDK에 비해 CDK9에 대해 최소 22배 더 선택적인 강력하고 선택적인 CDK9-사이클린 T1 억제제입니다. (rel)-MC180295는 또한 GSK-3α를 억제하고; 및 GSK-3β (rel)-MC180295((rel)-(rel)-MC180295)는 강력한 항종양 효과가 있습니다.
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Cas No.: 2237942-08-2
Sample solution is provided at 25 µL, 10mM.
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(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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