An inhibitor of the catalytic PARP domain of TNKS1/2 that blocks canonical Wnt signaling with an IC50 value of 790 nM; decreases β-catenin levels in colorectal cancer (CRC) cells

JW 74 – 5 mg

Brand:
Cayman
CAS:
863405-60-1
Storage:
-20
UN-No:
Non-Hazardous - /

Tankyrases (TNKS) are poly(ADP-ribose) polymerases (PARPs) that cleave NAD+ to produce nicotinamide and ADP-ribose, which is then covalently attached to an acceptor protein in a process known as poly(ADP-ribosyl)ation. TNKS have key roles in the Wnt signaling pathway as part of the β-catenin destruction complex. JW 74 is an inhibitor of the catalytic PARP domain of TNKS1/2 that blocks canonical Wnt signaling with an IC50 value of 790 nM.{30990,30991} It increases the levels of Axin2 and decreases β-catenin levels in colorectal cancer (CRC) cells, leading to down-regulation of Wnt target genes.{30991} JW 74 inhibits the growth of CRC xenograft tumors in mice.{30991} JW 74 induces apoptosis and differentiation in osteosarcoma cell lines.{30990}  

 

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Description

An inhibitor of the catalytic PARP domain of TNKS1/2 that blocks canonical Wnt signaling with an IC50 value of 790 nM; decreases β-catenin levels in colorectal cancer (CRC) cells, leading to down-regulation of Wnt target genes; inhibits the growth of CRC xenograft tumors in mice

Formal name: 4-[4-(4-methoxyphenyl)-5-[[[3-(4-methylphenyl)-1,2,4-oxadiazol-5-yl]methyl]thio]-4H-1,2,4-triazol-3-yl]-pyridine

Synonyms: 

Molecular weight: 456.5

CAS: 863405-60-1

Purity: ≥98%

Formulation: A crystalline solid

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

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