Г007-ЛК

Общее описание

A cell-permeable, triazolyl-vinyl-oxadiazole compound that targets adenosine site of the NAD⁺ pocket in the TNKS PARP domain and acts as a potent and highly selective tankyrase inhibitor (IC₅₀ = 33 and 26 nM, respectively, against TNKS1/PARP5a/ARTD5 and TNKS2/PARP5b/ARTD6 in auto-PARsylation assays), effectively inhibiting murine Wnt3a-induced reporter activity in human HEK293 and murine 10T1/2 cultures (IC_max ~300 and 600 nM, respectively). Shown to display little or no inhibitory potency (IC₅₀ >10 μM) toward 7 other PARP enzymes (PARP1, 2, 3, 6, 7,10,11), 90 kinases, 16 phosphatases, and 75 GPCRs (IC₅₀ >10 μM). Shown to inhibit two CRC lines, COLO-320DM & SW403, colony formation in vitro (200 nM) and tumor expansion in mice in vivo (20 mg/kg via daily i.p.), although G007-LK toxicity is observed at higher dosages (≥30 mg/kg/12 h or 60 mg/kg/d via i.p.).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Биохимия/физиол Действия

Cell permeable: yes