store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CCT251545 is an potent and oral-bioavailable WNT signaling inhibitor(IC50 of 5 nM in 7dF3 cells).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 41.00 | |
2 mg | In stock | $ 57.00 | |
5 mg | In stock | $ 90.00 | |
10 mg | In stock | $ 157.00 | |
25 mg | In stock | $ 297.00 | |
50 mg | In stock | $ 571.00 | |
100 mg | In stock | $ 819.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 90.00 |
Description | CCT251545 is an potent and oral-bioavailable WNT signaling inhibitor(IC50 of 5 nM in 7dF3 cells). |
Targets&IC50 | WNT (7dF3 cells):5 nM |
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]. |
Molecular Weight | 421.92 |
Formula | C23H24ClN5O |
CAS No. | 1661839-45-7 |
store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45mg/ml (106.66 Mm)
You can also refer to dose conversion for different animals. More
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CCT251545 1661839-45-7 Cytoskeletal Signaling Stem Cells Wnt/beta-catenin inhibit Wnt Inhibitor CCT 251545 CCT-251545 inhibitor