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Chemical Structure : CDK-TCIP1
Catalog No.: 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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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).
| M.Wt | 1020.66 | |
| Formula | C48H62ClN11O8S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Sarott RC, et al. Science. 2024 Oct 4;386(6717):eadl5361.
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