CCT251545

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Clon N/A
Menge 50mg
ArtNr HY-12681-50mg
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
Synonyms
CCT 251545, CCT-251545
CAS No.
1661839-45-7
Purity
>98%
MW
4219225
Formula
C23H24ClN5O
Solubility
DMSO: >= 50 mg/mL
Biological Description
CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with IC50 value of 5 nM.
IC50 value: 5 nM [2]
Target: WNT
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. [1] CCT251545 demonstrates weak inhibition of tankyrase enzymes (TNKS1 IC50 > 10 uM, TNKS2 IC50 = 15.0 +/- 0 uM). 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 uM and 0.190 +/- 0.030 uM, respectively) and demonstrated potent inhibition of WNT3a ligand-dependent reporter readout in PA-1 cells (IC50 = 0.007 uM).[2]
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. [1]
Free  Sample
Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 50mg
Lieferbar: In stock
Listenpreis: 733,57 €
Rabatt: -10,0%
Preis: 660,21 €
Sie sparen: 73,36 €
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