XAV-939 Inhibitor CAS No. 284028-89-3

Cat. No.	Name	Size	Price
KI0416	XAV-939	10 mg	$112
	XAV-939	25 mg	$272
	XAV-939	50 mg	$432
	XAV-939	200 mg	$1232

Chemical Characteristic

Product Name	XAV-939
CAS No.	284028-89-3
Molecular Weight	312.31
Formula	C₁₄H₁₁F₃N₂OS
Chemical Name	3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one
Smiles	c1(nc2c(c(=O)[nH]1)CSCC2)c1ccc(cc1)C(F)(F)F
Chemical Structure

Biological activities

XAV-939 is a small-molecule tankyrase (TNKS) inhibitor.^[1] XAV-939 strongly prevents TNKS1 and TNKS2, with IC50 of 11 and 4 nM, respectively. However, XAV-939 reveals much weaker affects on Poly (ADP-ribose) polymerase 1 (PARP1) and PARP2. XAV-939 binds tightly to the catalytic (PARP) domains of TNKS1 and TNKS2 with K_{d of 99 and 93 nM, respectively. XAV-939 also binds to recombinant PARP1, although with a significantly lower binding affinity with a K_{d of 1.2 μM. XAV-939 promotes axin-Gsk3β interactions and thereby represses canonical Wnt signaling. XAV-939 selectively inhibits beta-catenin-mediated transcription. XAV-939 stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex. XAV-939 stabilizes axin by suppressing the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2. XAV-939 strongly prevents Wnt3a-stimulated Super-Topflash (STF) activity in HEK293 cells, but does not affect CRE, NF-κB or TGF-β luciferase reporters. XAV-939 treatment inhibits Wnt3a-induced accumulation of β-catenin in HEK293 cells. XAV-939 also prevents STF activity in SW480 cells, a colorectal cancer cell line harbouring a truncated APC (adenomatous polyposis coli). XAV-939 significantly increases β-catenin phosphorylation (S33/S37/T41) in SW480 cells. XAV-939 blocks not only TNKS binding at 0.1 μM but also PARP1/2 binding at 1 μM.^[2] XAV-939 dramatically decreases DNA-PKcs protein levels. Treatment of human lymphoblasts with 1.0 μM XAV-939 leads to a significant increase of tankyrase 1 levels over DMSO treated controls.^[3]}}

References

[1] Kirby CA, et al. Structure of human tankyrase 1 in complex with small-molecule inhibitors PJ34 and XAV-939. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2012, 68(Pt 2): 115-118. [2] Huang SM, et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature. 2009, 461(7264): 614-620. [3] Dregalla RC, et al. Regulatory roles of tankyrase 1 at telomeres and in DNA repair: suppression of T-SCE and stabilization of DNA-PKcs. Aging (Albany NY). 2010, 2(10): 691-708.

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