CCT251545

SKU: orb1308477

Description

CCT251545

Research Area

Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1661839-45-7
• MW: 421.92
• Purity: 99.73% (May vary between batches)
• Formula: C₂₃H₂₄ClN₅O
• SMILES: Cn1cc(cn1)-c1ccc(cc1)-c1cncc(Cl)c1N1CCC2(CCNC2=O)CC1
• Target: Wnt/beta-catenin
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.37 mM);DMSO:1 mg/mL (2.37 mM)

Bioactivity

• Target IC50:
  WNT (7dF3 cells):5 nM
• In Vivo:
  In vivo, CCT251545 with WNT-dependent tumors activity.
• 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.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

betacatenin, beta-catenin, CCT 251545, CCT251545, CCT-251545, bcatenin, inhibit, Inhibitor, Wnt/β-catenin, Wnt, Wnt/betacatenin, Wnt/b-catenin, WNT, 7dF3 cells, βcatenin

Compound Identifiers

PubChem CID

77050682