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CAS No.: 2118356-96-8

CDK9 PROTAC compound 3 Catalog No. CSN22310

Synonyms: CDK9-PROTAC

PROTAC CDK9 Degrader-1 is a CRBN-recruiting PROTAC selectively targeting on CDK9, consist of a CDK9 ligand (aminopyrazole analog) linked to a CRBN E3 ligand thalidomide.

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生物活性

描述PROTAC CDK9 Degrader-1 is a CRBN-recruiting PROTAC selectively targeting on CDK9, consist of a CDK9 ligand (aminopyrazole analog) linked to a CRBN E3 ligand thalidomide. Treatment with PROTAC CDK9 Degrader-1 led to a degradation of CDK9 by ~56% and ~65%, but not CDK2 or 5, at concentration of 10 and 20μM in HCT116 cells. Both of the phosphorylation status of Ser2 on RPB1, a direct substrate of CDK9, and the protein level of pro-survival protein Mcl-1 of which activity was regulated by CDK9, were decreased due to the degradation of CDK9 by addition of 10 or 20μM PROTAC CDK9 Degrader-1^[1].
参考文献

[1] Robb CM, Contreras JI, et al. Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC). Chem Commun (Camb). 2017 Jul 4;53(54):7577-7580.

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
- 1.6296 mL
- 8.1478 mL
- 16.2957 mL
- 5 mM
- 0.3259 mL
- 1.6296 mL
- 3.2591 mL
- 10 mM
- 0.1630 mL
- 0.8148 mL
- 1.6296 mL

技术信息

CAS号	2118356-96-8	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C33H35N5O7	运输	蓝冰
分子量	613.66	别名	CDK9-PROTAC

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CDK9 PROTAC compound 3 Catalog No. CSN22310

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