|(S)-3-(4-丙烯酰胺苯甲酰胺)-N-(2-(二甲基氨基)-1-苯基乙基)-6,6-二甲基-4,6-二氢吡咯并[3,4-c]吡唑-5(1H)-甲酰胺|CsnPharm

CAS No.: 1957203-01-8

YKL-5-124 Catalog No. CSN28803

YKL-5-124 is a highly selective, covalent CDK7 inhibitor with IC50 value of 9.7nM. It causes arrest at the G1/S transition and inhibition of E2F-driven gene expression, but resulted in no change to Pol II CTD phosphorylation.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Cyclin-dependent kinase 7 (CDK7), along with cyclin H and MAT1, forms the CDK-activating complex (CAK), which directs progression through the cell cycle via T-loop phosphorylation of cell cycle CDKs^[1].'YKL-5-124, a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for CDK7/Mat1/CycH, CDK2 and CDK9 respectively, displays biochemical and cellular selectivity for CDK7 over CDK12/13^[2].YKL-5-124 robustly inhibited CDK1 and CDK2 T-loop phosphorylation in a representative panel of SCLC lines at concentrations as low as 50 nM. a significant increase in TNF and CXCL10 expression was detected after YKL-5-124 treatment in the WT cells but not in the C312S mutant cells. YKL-5-124 demonstrated notably delayed tumor growth in the RP and RPP-MYC .Remarkably, YKL-5-124 significantly prolonged survival, with an added median survival benefit of approximately 30 days in both RPP and RP models^[3]. Selective CDK7 inhibition with YKL-5-124 is sufficient to reduce the phosphorylation levels of CDK1 and CDK2 but not that of RNA Pol II CTD.Furthermore, YKL-5-124 treatment had no effect on expression of superenhancer (SE)-associated genes including INSM1,ASCL1, NFIB, and MYC^[4].
参考文献

[1] Georgina P Sava, Hailing Fan,et al. CDK7 inhibitors as anticancer drugs. Cancer Metastasis Rev. 2020 Sep;39(3):805-823.
[2] Calla M Olson, Yanke Lianget al. Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype. Cell Chem Biol. 2019 Jun 20;26(6):792-803.e10.
[3] Hua Zhang , Camilla L Christensen,et al. CDK7 Inhibition Potentiates Genome Instability Triggering Anti-tumor Immunity in Small Cell Lung Cancer. Cancer Cell. 2020 Jan 13;37(1):37-54.e9.
[4] Camilla L. Christensen, Nicholas Kwiatkowski, Brian J,et al. Targeting Transcriptional Addictions in Small Cell Lung Cancer with a Covalent CDK7 Inhibitor. Volume 26, Issue 6, 8 December 2014, Pages 909-922.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9395 mL
- 9.6973 mL
- 19.3946 mL
- 5 mM
- 0.3879 mL
- 1.9395 mL
- 3.8789 mL
- 10 mM
- 0.1939 mL
- 0.9697 mL
- 1.9395 mL

技术信息

CAS号	1957203-01-8	储存条件	粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C28H33N7O3	运输	蓝冰
分子量	515.61	别名

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

YKL-5-124 Catalog No. CSN28803

靶点选择性

请登录您的专属账户

确认信息