A TNKS2 inhibitor (IC50 = 6 nM); inhibits Wnt ligand-induced signaling in an HEK293 cell reporter assay (IC50 = 3.5 nM); reduces Axin 2 mRNA expression in MMTV-Wnt1 tumor bearing mice

NVP-TNKS656 – 1 mg

Brand:
Cayman
CAS:
1419949-20-4
Storage:
-20
UN-No:
De Minimis - 3077 / 9

NVP-TNKS656 is an orally bioavailable inhibitor of tankyrase 2 (TNKS2; IC50 = 6 nM).{40669} It is selective for TNKS2 over poly(ADP-ribose) polymerase (PARP) 1 and 2 (IC50s = >19 and 32 nM, respectively). NVP-TNKS656 inhibits Wnt ligand-induced signaling with an IC50 value of 3.5 nM in an HEK293 cell reporter assay. In vivo, NVP-TNKS656 (350 mg/kg) reduces Axin 2 mRNA expression, a Wnt/β-catenin target gene, in MMTV-Wnt1 tumor bearing mice.  

 

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Description

A TNKS2 inhibitor (IC50 = 6 nM); inhibits Wnt ligand-induced signaling in an HEK293 cell reporter assay (IC50 = 3.5 nM); reduces Axin 2 mRNA expression in MMTV-Wnt1 tumor bearing mice,

Formal name: N-(cyclopropylmethyl)-4-(4-methoxybenzoyl)-N-[(3,5,7,8-tetrahydro-4-oxo-4H-pyrano[4,3-d]pyrimidin-2-yl)methyl]-1-piperidineacetamide

Synonyms: 

Molecular weight: 494.6

CAS: 1419949-20-4

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||Research Area|Cell Biology|Cell Signaling|Wnt Signaling

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