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XAV939

Cayman Chemical Item Number 13596

(CAS 284028-89-3)

XAV939 (CAS 284028-89-3)

See more	Inhibitors (475) Cancer (556) Signal Transduction (302)

Description

The Wnt signaling pathway is integral to normal biological processes and inappropriately active in many cancers. It is regulated through degradation of the downstream effector β-catenin via a complex consisting of the tumor suppressor APC, axin, and glycogen synthase kinase 3 (GSK3). Axin is the concentration-limiting factor for this degradation complex. Initially indentified as telomere-associated proteins¹, tankyrases promote axin ubiquitination, possibly through poly-ADP-ribosylation (PARsylation).² XAV939 is a potent, small molecule inhibitor of tankyrase (TNKS) 1 and 2 with IC₅₀ values of 11 and 4 nM, respectively.² By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480 cells.² At concentrations as low as 0.33 µM, XAV939 inhibits colony formation of APC-deficient colorectal cancer cells.²

1 Smith, S., Giriat, I., Schmitt, A., et al. Tankyrase, a poly(ADP-ribose) polymerase at human telomeres. Science 282 1484-1487 (1998 Nov).

2 Huang, S.A., Mishina, Y.M., Liu, S., et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature 461 614-619 (2009).

Formal Name	3,?5,?7,?8-?tetrahydro-?2-?[4-?(trifluoromethyl)phenyl]-?4H-?thiopyrano[4,?3-?d]pyrimidin-?4-?one
CAS Number	284028-89-3
Molecular Formula	C₁₄H₁₁F₃N₂OS
Formula Weight	312.3
Formulation	A crystalline solid
Purity	≥98%
Stability	2 years
Storage	-20°C
Shipping	Wet ice in continental US; may vary elsewhere
SMILES	OC1=NC(C2=CC=C(C(F)?(F)?F)?C=C2)?=NC3=C1CSCC3

Background Reading

Huang, S.A., Mishina, Y.M., Liu, S., et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature 461 614-619 (2009).

Smith, S., Giriat, I., Schmitt, A., et al. Tankyrase, a poly(ADP-ribose) polymerase at human telomeres. Science 282 1484-1487 (1998 Nov).

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