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CAS No.: 2139287-33-3

THAL-SNS-032 Catalog No. CSN22287

Synonyms: THAL-SNS-032

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.

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生物活性

实验方案

技术信息

生物活性

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].
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.

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
- 1.1507 mL
- 5.7536 mL
- 11.5072 mL
- 5 mM
- 0.2301 mL
- 1.1507 mL
- 2.3014 mL
- 10 mM
- 0.1151 mL
- 0.5754 mL
- 1.1507 mL

技术信息

CAS号

2139287-33-3

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C40H52N8O10S2

运输

蓝冰

分子量

869.02

别名

THAL-SNS-032

溶解度

DMSO	100.0 mg/mL (115.1 mM)
Water	Insoluble
Ethanol	30.0 mg/mL (34.5 mM)

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