xav-939
Synonym(s):3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one
- CAS NO.:284028-89-3
- Empirical Formula: C14H11F3N2OS
- Molecular Weight: 312.31
- MDL number: MFCD00106866
- EINECS: 687-302-1
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is xav-939?
Description
XAV-939 (284028-89-3) is a tankyrase inhibitor (IC50=11 and 4 nM for TNKS1 and 2 respectively).? Antagonizes wnt signaling via stimulation of β-catenin degradation and stabilization of actin.1? XAV-939 robustly induces cardiomyogenesis of stem cells.2? Cell permeable
The Uses of xav-939
A tankyrase (TNKS) inhibitor that antagonizes Wnt signaling via stimulation of β-catenin degradation and stabilization of axin. It inhibits proliferation of the μ-catenin-dependent colon carcinoma cell line DLD-1.
The Uses of xav-939
XAV939 has been used in the inhibition
- of tankyrase in neuroblastoma cell lines
- of diphtheria toxin-like ADP-ribosyltransferases (ARTD) in medulloblastoma cells
- of wnt signalling in human induced pluripotent stem cells (hiPSCs)
What are the applications of Application
XAV939 is a potent inhibitor of beta-catenin, TNKS1, and TNKS2
Definition
ChEBI: XAV939 is a thiopyranopyrimidine in which a 7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine skeleton is substituted at C-4 by a hydroxy group and at C-2 by a para-(trifluoromethyl)phenyl group. It has a role as a tankyrase inhibitor. It is a thiopyranopyrimidine and a member of (trifluoromethyl)benzenes.
Biochem/physiol Actions
XAV939 is a cell-permeable dihydrothiopyranopyrimidinol, which elicits anti-tumor functionality against colon, lung, breast and liver cancer. It binds to catalytic poly-ADP-ribose polymerase (PARP) domain of the tankyrase enzyme resulting in β-catenin destruction. It also inhibits tankyrase in neuroblastoma promoting apoptosis in tumor cells.
storage
Room temperature
References
1) Huang?et al. (2009),?Tankyrase inhibition stabilizes axin and antagonizes Wnt signaling; Nature,?46?614 2) Wang?et al. (2011),?Cardiac induction of embryonic stem cells by a small molecule inhibitor of Wnt/β-catenin signaling; Chem. Biol.,?6?192
Properties of xav-939
Boiling point: | 429.3±55.0 °C(Predicted) |
Density | 1.5 |
Flash point: | 213.4℃ |
storage temp. | room temp |
solubility | DMSO: soluble5mg/mL, clear |
form | powder |
pka | 0.23±0.20(Predicted) |
color | white to beige |
Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
Safety information for xav-939
Signal word | Danger |
Pictogram(s) |
Skull and Crossbones Acute Toxicity GHS06 |
GHS Hazard Statements |
H301:Acute toxicity,oral H319:Serious eye damage/eye irritation |
Precautionary Statement Codes |
P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for xav-939
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