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Merck
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Key Documents

575545

Sigma-Aldrich

XAV939

≥97% (HPLC), solid, Tankyrase1/2 inhibitor, Calbiochem

Sinónimos:

Tankyrase1/2 Inhibitor, XAV939, 2-(4-(Trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-ol, Wnt Pathway Inhibitor V, TNKS1/2 Inhibitor I

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About This Item

Fórmula empírica (notación de Hill):
C14H11F3N2OS
Peso molecular:
312.31
UNSPSC Code:
12352200
NACRES:
NA.54

product name

Tankyrase1/2 Inhibitor, XAV939, The Tankyrase1/2 Inhibitor, XAV939 controls the biological activity of Tankyrase1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Quality Level

100

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 25 mg/mL

shipped in

ambient

storage temp.

−20°C

General description

A cell-permeable dihydrothiopyranopyrimidinol that binds TNKS1/PARP5a and TNKS2/PARP5b with high affinity (Kd = 99 and 93 nM, respectively) and potently inhibits their PARsylation (poly ADP-ribosylation) activity (IC50 = 11 and 4 nM, respectively), while exhibiting much lower activity against PARP1 and PARP2 (IC50 = 2.194 and 0.114 µM, respectively). TNKS, but not PARP1/2, function knockdown by siRNA or XAV939 treatment suppresses cellular axin1/2 PARsylation and ubiquitination/proteasomal degradation, resulting in axin build-up, β-catenin destruction, and blockage of Wnt signaling. XAV939 is shown to inhibit the growth of β-catenin-dependent DLD-1, but not that of β-catenin-independent RKO, cells (by >95% vs. no effect at 3.3 µM, respectively) in vitro and prevent the regeneration of zebrafish tail fin (by ~70% at 7 d post-amputation, 5 µM) after surgical removal in vivo.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Huang, S.M., et al. 2009. Nature461, 614.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302

Hazard Classifications

Acute Tox. 4 Oral

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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