CDK-TCIP1

Chemical Structure : CDK-TCIP1

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货号: PC-23150Not For Human Use, Lab Use Only.

CDK-TCIP1 is a bivalent molecule linking CDK9 inhibitor SNS-032 to BCL6 ligand BI3812, potently and specifically kills BCL6-overexpressing cells with EC50 of 7.7 nM for SUDHL5 cells.

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生物&药学活性

CDK-TCIP1 is a bivalent molecule linking CDK9 inhibitor SNS-032 to BCL6 ligand BI3812, activates BCL6-regulated transcription, potently and specifically kills BCL6-overexpressing cells with EC50 of 7.7 nM for SUDHL5 cells.
CDK-TCIP1 shows 55 times greater cytotoxicity than the effect of the CDK9 and BCL6 parental inhibitors.
CDK-TCIP1 is uniquely potent in DLBCL lines dependent on having high levels of BCL6 expression due to oncogenic mutations in the BCL6 gene or its regulatory regions.
CDK-TCIP1 functions by ternary complex formation and relocalization of CDK9 activity to BCL6 on chromatin.
CDK-TCIP1 forms a ternary complex between purified BCL6BTB and CDK9-CycT1 with EC50 of 11 nM, activates BCL6-controlled GFP expression in DLBCL cells, with a comparable EC50 of 58 nM.
CDK-TCIP1 selectively recruit CDK9 and its activity to BCL6-repressed genetic loci.
CDK-TCIP1 significantly increases the expression of pro-apoptotic, BH3 (BCL2 homology 3)-domain containing, BCL6-target genes in mRNA, including BBC3 (BCL2-interacting protein 3; also called PUMA for p53-upregulated modulator of apoptosis) and PMAIP1 (also called NOXA), as well as the cell cycle arrest gene CDKN1B (p27).

物理化学性质&存储条件

分子量	1020.66
分子式	C48H62ClN11O8S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(5-(((5-(tert-butyl)oxazol-2-yl)methyl)thio)thiazol-2-yl)-1-(7-(1-(5-chloro-4-((8-methoxy-1-methyl-3-(2-(methylamino)-2-oxoethoxy)-2-oxo-1,2-dihydroquinolin-6-yl)amino)pyrimidin-2-yl)piperidine-4-carboxamido)heptanoyl)piperidine-4-carboxamide

参考文献

1. Sarott RC, et al. Science. 2024 Oct 4;386(6717):eadl5361.

CDK-TCIP1

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CDK-TCIP1

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