XAV-939

Short Summary : Tankyrase 1/2 inhibitor

Category : DNA Damage/DNA Repair|PARP

Purity : 0.98

CAS Number : 284028-89-3

Formula : C14H11F3N2OS

Molecular Weight : 312.31

SMILE : C1CSCC2=C1NC(=NC2=O)C3=CC=C(C=C3)C(F)(F)F

Solubility : >15.6mg/mL in DMSO

Storage : Store at -20°C

Description : XAV-939 is a small-molecule inhibitor of tankyrase 1/2 with IC50 values of 4 and 11 nM, respectively [1].XAV-939 was screened out as an inhibitor of Wnt/-catenin pathway. In HEK293 cells, XAV-939 significantly inhibited the Wnt3a-stimulated STF activity and -catenin accumulation. In SW480 cells, XAV-939 also inhibited STF activity and increased -catenin phosphorylation. XAV-939 was demonstrated to stabilize the axin levels through inhibiting tankyrases and subsequently inhibit the Wnt signaling. It tightly bound to the catalytic domains of tankyrase 1 and tankyrase 2 with Kd values of 99 and 93 nM, respectively. In addition, XAV-939 significantly inhibited colony formation of -catenin-dependent DLD-1 cells but not -catenin-independent RKO cells [1].References:[1] Huang S M A, Mishina Y M, Liu S, et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature, 2009, 461(7264): 614-620.

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