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THAL-SNS-032

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Chemical Structure| 2139287-33-3 同义名 : -
CAS号 : 2139287-33-3
货号 : A160834
分子式 : C40H52N8O10S2
纯度 : 99%+
分子量 : 869.019
MDL号 : MFCD31689257
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(120.83 mM)，配合低频超声助溶，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
靶点

  • CRBN
描述 THAL-SNS-032 is a selective PROTAC, consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN), targeting on CDK9. Treatment with THAL-SNS-032 led a completely deletion of CDK9 at concentration of 250nM, 500nM and 1μM, but 5μM or 10μM, post 6-hour treatment in MOLT 4 cells. A significant degradation of CDK9 could be observed by 250nM THAL-SNS-032 post 1-8h, but a decrease of CDK1, 2 could be observed post 16 hours. THAL-SNS-032 exhibits CRBN-dependent anti-proliferative with IC50 value of 3.63μM post 72h and led pro-apoptotic effects shown by cleaved PARP and Caspase-3 at concentration of 250nM post 4-24h in MOLT 4 cells. The depletion of CDK9 by 250nM THAL-SNS-032 exhibits transcriptional effects consistent with a selective CDK9 inhibitor and diminished elongating polymerase II. An inhibition of phosphorylation on serine 2 of the CTD of RNA Pol II could be observed[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.15mL

0.23mL

0.12mL

5.75mL

1.15mL

0.58mL

11.51mL

2.30mL

1.15mL
参考文献

[1]Olson CM, Jiang B, et al. Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nat Chem Biol. 2018 Feb;14(2):163-170.