A small molecule inhibitor of tankyrase 1 and 2 (IC50 = 11 and 4 nM

XAV939 – 10 mg

Brand:
Cayman
CAS:
284028-89-3
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

The Wnt signaling pathway is integral to normal biological processes and inappropriately active in many cancers. It is regulated through degradation of the downstream effector β-catenin via a complex consisting of the tumor suppressor APC, axin, and glycogen synthase kinase 3 (GSK3). Axin is the concentration-limiting factor for this degradation complex. Initially indentified as telomere-associated proteins{6770}, tankyrases promote axin ubiquitination, possibly through poly-ADP-ribosylation (PARsylation).{17502} XAV939 is a potent, small molecule inhibitor of tankyrase (TNKS) 1 and 2 with IC50 values of 11 and 4 nM, respectively.{17502} By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480 cells.{17502} At concentrations as low as 0.33 µM, XAV939 inhibits colony formation of APC-deficient colorectal cancer cells.{17502}  

 

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Description

A small molecule inhibitor of tankyrase 1 and 2 (IC50 = 11 and 4 nM, respectively); increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin; inhibits colony formation of APC-deficient colorectal cancer cells at 0.33 µM

Formal name: 3,5,7,8-tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one

Synonyms: 

Molecular weight: 312.3

CAS: 284028-89-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Signaling|Wnt Signaling||Research Area|Cancer|Transcription Factors||Research Area|Cell Biology|Cell Signaling|Wnt Signaling

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