XAV939---Wnt Antagonist

XAV939 is a potent and selective Wnt pathway antagonist. It functions to stabilize Axin by inhibiting the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2 with IC50 of 11 nM and 4 nM, respectively. It has been used to study Wnt-dependent cancers. In addition, XAV939 was shown to stabilize Axin2 level in oligodendrocyte precursor cells in the spinal cord and accelerated their differentiation and myelination after hypoxic and demyelinating injury. It can also robustly induce cardiomyocyte differentiation from mouse and human ESCs/iPSCs.

Product information

CAS Number: 284028-89-3

Molecular Weight: 312.31

Formula: C14H11F3N2OS

Synonym:

NVP-XAV939

Chemical Name: 2-(4-(trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-ol

Smiles: OC1=NC(=NC2CCSCC=21)C1C=CC(=CC=1)C(F)(F)F

InChiKey: KLGQSVMIPOVQAX-UHFFFAOYSA-N

InChi: InChI=1S/C14H11F3N2OS/c15-14(16,17)9-3-1-8(2-4-9)12-18-11-5-6-21-7-10(11)13(20)19-12/h1-4H,5-7H2,(H,18,19,20)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 50 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: Powder: 4^oC 1 year. DMSO: 4^oC 3 month; -20^oC 1 year.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

XAV939 was used at 1 µM concentration to stabilize Axin and in stem cell culture. It can be used to functionally replace Dkk protein in blocking Wnt signaling in many assay conditions (e.g., 40 times more effective in inducing cardiogenesis than recombinant Wnt inhibitor protein Dkk).

References:

1. Huang SMA, et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signaling; (2009) Nature. 461, 614-620
2. Wang H, et al. Cardiac induction of embryonic stem cells by a small molecule inhibitor of Wnt/β-catenin signaling. (2011) ACS Chem Biol. 6(2):192-7.
3. Fancy SP, et al. Axin2 as regulatory and therapeutic target in newborn brain injury and remyelination. (2011) Nat Neurosci. 14(8):1009-16.
4. Willems E, et al. Small-molecule inhibitors of the Wnt pathway potently promote cardiomyocytes from human embryonic stem cell-derived mesoderm. (2011) Circ Res.109(4):360-4.

Products are for research use only. Not for human use.

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