XAV-939

284028-89-3

C14H11F3N2OS

DMSO : 21.5 mg/mL (68.84 mM; Need ultrasonic and warming)

Epigenetics; Cell Cycle/DNA Damage; Stem Cell/Wnt

XAV-939 is a tankyrase (TNKS) inhibitor and an indirect inhibitor of Wnt/beta-catenin signaling, with IC₅₀s of 5 and 2 nM for TNKS1 and TNKS2, respectively. IC50 & Target: IC50: 5 nM (TNKS1), 2 nM (TNKS2)^[6] In Vitro: XAV939 (1 uM) strongly inhibis STF activity in SW480 cells, Wnt3a-stimulated STF activity in HEK293 cells, but does not affect CRE, NF-kappaB or TGF-beta luciferase reporters. XAV939 regulates axin levels through tankyrase inhibition in HEK293 cell^[1]. XAV939 (0.5 uM, 1.0 uM) reduces DNA-PKcs protein levels 50% of the relative DMSO control in human lymphoblasts^[2]. XAV939 induces a second wave of pro-cardiomyocyte gene expression as shown by increased Mesp1 and Isl1expression 2 to 4 days after Wnt inhibition, and by increased Nkx2.5 expression 4 to 6 days after XAV939 addition^[3]. XAV-939 (10 nM) has a suppressive effect on elevated MMP-13 levels in both IL-1beta-induced SW 1353 cells^[4]. In Vivo: XAV-939 (3 mL, 10 nM) has a suppressive effect on elevated MMP-13 levels in the rat OA model^[4]. XAV-939 (1 mg/mL, i.p.) ameliorates the psoriasiform skin disease induced by IMQ. XAV-939 results in a significant decrease in the IMQ-induced epidermal hyperplasia (indicated by acanthosis) and dermal inflammatory infiltrates in mice^[5].