CCT251545|cas 1661839-45-7|DC Chemicals

Cas No.:	1661839-45-7
Chemical Name:	CCT251545
Synonyms:	CCT251545;CCT-251545
SMILES:	O=C1C2(CCN(C3C(C4C=CC(C5C=NN(C)C=5)=CC=4)=CN=CC=3Cl)CC2)CCN1
Formula:	C₂₃H₂₄ClN₅O
M.Wt:	421.922563552856
Purity:	>98%
Sotrage:	4°C for 1 year, -20°C for more than 2 years

Description:

CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with IC50 value of 5 nM. in vitro: CCT251545 is a potent and selective chemical probe for the human Mediator complex-associated protein kinases CDK8 and CDK19 with >100-fold selectivity over 291 other kinases. CCT251545 also reduces phospho-STAT1SER727 levels in SW620 cells with IC50 of 9 nM. CCT251545 is a small-molecule inhibitor of the WNT pathway discovered through cell-based screening. CCT251545 displays potent cell-based activity. CCT251545 alters WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1. CCT251545 demonstrates weak inhibition of tankyrase enzymes (TNKS1 IC50 > 10 μM, TNKS2 IC50 = 15.0 ± 0 μM). CCT251545 potently inhibits reporter-based readouts of basal WNT pathway activity in LS174T and SW480 cells in the absence of WNT ligand or other stimulants (IC50 = 0.023 ± 0.011 μM and 0.190 ± 0.030 μM, respectively) and demonstrated potent inhibition of WNT3a ligand-dependent reporter readout in PA-1 cells (IC50 = 0.007 μM) in vivo: CCT251545 as a potent and selective chemical probe suitable for cell-based exploration of the reported context-dependent roles of CDK8 and CDK19 and associated kinase module subunits in human disease and other biological settings.

Cat. No.	Product name	Field of application
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