| Name | CCT251545 |
| Description | CCT251545 is an potent and oral-bioavailable WNT signaling inhibitor(IC50 of 5 nM in 7dF3 cells). |
| In vitro | CCT251545, a small-molecule inhibitor of the WNT pathway discovered through cell-based screening, 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.?X-ray crystallography demonstrates a type 1 binding mode involving insertion of the CDK8 C terminus into the ligand binding site.?In contrast to type II inhibitors of CDK8 and CDK19, CCT251545 displays potent cell-based activity.?We show that CCT251545 and close analogs alter WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1.?Consistent with this, we find that phosphorylation of STAT1(SER727) is a biomarker of CDK8 kinase activity in vitro and in vivo[1]. |
| In vivo | In vivo, CCT251545 with WNT-dependent tumors activity[1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.37 mM), Sonication is recommended.
DMSO : 1 mg/mL (2.37 mM), Sonication is recommended.
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| Keywords | βcatenin | Wnt/β-catenin | Wnt/betacatenin | Wnt/b-catenin | WNT, 7dF3 cells | Wnt | Inhibitor | inhibit | CCT-251545 | CCT251545 | CCT 251545 | beta-catenin | betacatenin | bcatenin |
| Inhibitors Related | Chlorquinaldol | Urea | Wnt pathway activator 1 | Neohesperidin | XAV-939 | Ethyl linoleate | Monensin sodium salt | Nimbolide | Isoquercetin | (±)-Nornicotine | Methyl Vanillate | Bisdemethoxycurcumin |
| Related Compound Libraries | Neural Regeneration Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Hematonosis Compound Library | Neuroprotective Compound Library | Inhibitor Library | Orally Active Compound Library | Bioactive Compounds Library Max | Cytoskeletal Signaling Pathway Compound Library | Wnt/Hedgehog/Notch Compound Library | Anti-Liver Cancer Compound Library | Neuronal Differentiation Compound Library |
United States
