A potent and selective inhibitor of TNKS1 and TNKS2 (IC50s = 26 and 15 nM

WIKI4 – 5 mg

Brand:
Cayman
CAS:
838818-26-1
Storage:
-20
UN-No:
Non-Hazardous - /

Tankyrases (TNKS) cleave NAD+ to produce nicotinamide and ADP-ribose, which is then covalently attached to an acceptor protein in the process known as poly(ADP-ribosyl)ation. WIKI4 is a potent and selective inhibitor of TNKS1 and TNKS2 (IC50s = 26 and 15 nM, respectively).{27316,27317} It has little or no effect on related polymerases or transferases at 10 µM.{27317} Through its effects on TNKS2, WIKI4 prevents AXIN ubiquitinylation and degradation, blocking signaling through the Wnt/β-catenin pathway.{27316} WIKI4 inhibits the expression of β-catenin target genes and cellular responses to Wnt/β-catenin signaling in both cancer cell lines and embryonic stem cells.{27316}  

 

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Description

A potent and selective inhibitor of TNKS1 and TNKS2 (IC50s = 26 and 15 nM, respectively); blocks the expression of β-catenin target genes and cellular responses to Wnt/β-catenin signaling in both cancer cell lines and embryonic stem cells

Formal name: 2-[3-[[4-(4-methoxyphenyl)-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]thio]propyl]-1H-benz[de]isoquinoline-1,3(2H)-dione

Synonyms:  Tankyrase 1/2 Inhibitor V

Molecular weight: 521.6

CAS: 838818-26-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Signaling|Wnt Signaling||Research Area|Cancer|DNA Damage and Repair|PARP||Research Area|Cell Biology|Cell Signaling|Wnt Signaling||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System||Research Area|Cell Biology|Stem Cell Research

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