Description
An inhibitor of PARP1, PARP2, and TNKS1/2 (IC50s = 1, 1.2, and 50-11 nM, respectively); selective for PARP1, PARP2, and TNKS1/2 over PARP3 and PARP6-15 (IC50s = >3 μM); inhibits growth of DT40 cells in a PARP-dependent manner (IC50s = 3.2 and >15 μM for wild-type and PARP-/- cells, respectively); decreases expression of Wnt/β-catenin signaling pathway proteins in SW480 cells; enhances antitumor activity of temozolomide and carboplatin in a B16/F10 isograft model and MX-1 mouse xenograft model, respectively; inhibits tumor growth in a BRCA1 mutant MDA-MB-436 breast cancer mouse xenograft model at 30 and 100 mg/kg per day; delays hair regrowth in mice following hair removal,
Formal name: 8-[(1,3-dihydro-2H-isoindol-2-yl)methyl]-1,2-dihydro-3H-pyridazino[3,4,5-de]quinazolin-3-one
Synonyms:
Molecular weight: 317.3
CAS: 1140964-99-3
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Small Molecule Inhibitors|DNA Repair Enzymes||Research Area|Cancer|DNA Damage and Repair|PARP||Research Area|Cell Biology|Cell Signaling|Wnt Signaling||Research Area|Epigenetics, Transcription, & Translation|RNA, DNA, & Protein Synthesis