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(rel)-MC180295
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(rel)-MC180295图片
CAS NO:2237942-08-2
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
(rel)-MC180295 ((rel)-(rel)-MC180295) 是一种有效的选择性 CDK9-Cyclin T1 抑制剂,IC50 为 5 nM,对 CDK9 的选择性比其他 CDK 高至少 22 倍。 (rel)-MC180295 还抑制 GSK-3α;和 GSK-3β;。 (rel)-MC180295 ((rel)-(rel)-MC180295) 具有有效的抗肿瘤作用。
Cas No.2237942-08-2
别名(rel)-MC180295
Canonical SMILESNC1=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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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.