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CDK9 PROTAC compound 3

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Chemical Structure| 2118356-96-8 同义名 : PROTAC CDK9 Degrader-1
CAS号 : 2118356-96-8
货号 : A711157
分子式 : C33H35N5O7
纯度 : 99%+
分子量 : 613.66
MDL号 : MFCD31619245
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 100 mg/mL(162.96 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.63mL

0.33mL

0.16mL

8.15mL

1.63mL

0.81mL

16.30mL

3.26mL

1.63mL
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.