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MC180295

产品编号: DC12527 Featured
MC180295
结构式
2237942-08-2
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中国地区超过5000个高品质化合物库存
应用领域
MC180295 ((rel)-MC180295) 是一种有效、选择性的 CDK9-Cyclin T1 抑制剂，IC50 值为 5 nM，对其选择性至少是对其他 CDK 激酶 22 倍。MC180295 ((rel)-MC180295) 同时抑制 GSK-3α 和 GSK-3β。MC180295 具有的抗肿瘤活性。
化学性质生物活性化合物的使用COA & MSDS相关产品产品说明书
Cas No.: 2237942-08-2
名称: Rel-(4-amino-2-(((2S)-bicyclo[2.2.1]heptan-2-yl)amino)thiazol-5-yl)(2-nitrophenyl)methanone
别名: MC-180295;MC 180295
SMILES: C(C1SC(N[C@@H]2CC3CC2CC3)=NC=1N)(C1=CC=CC=C1[N+]([O-])=O)=O
分子式: C17H18N4O3S
分子量: 358.416
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: MC180295 (MC-180295, MC 180295) is a novel potent, highly selective CDK9 inhibitor with IC50 of 5 nM, displays >22-fold selectivity over other CDKs; also shows high selectivity against a panel of 250 kinases at 1 uM; specificly inhibits the phosphorylation levels of Ser2 (pSer2); CDK9-mediated phosphorylation of BRG1 prevents it from being recruited to heterochromatin loci, while CDK9 inhibition allows BRG1 to remodel chromatin and alter gene expression; demonstrates broad anti-cancer activity in vitro and is effective in in vivo cancer models; also sensitize to anti-PD1 in vivo, increases the numbers of CD45+ immune cells and the percentages of CD3+ T cells and activates dendritic cells in the tumor environment, while not kill human T lymphocytes and did not affect the ratio of CD4 and CD8 T cells in vivo.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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