XAV-939 [284028-89-3]

Catalog number: HY-15147_10mM
Brand: MedChem Express
Packing: 10 mM
Other sizes: 5 mg
10 mg
50 mg
100 mg
200 mg
Price: € 95.00
Expected delivery time: 10 days
Quantity:

Product specifications for - XAV-939 [284028-89-3]

Overview: 
Product group: Chemicals
Category: Inhibitors / activators
CAS No.: 284028-89-3
Properties: 
Purity: >98%
Molecular Formula: C14H11F3N2OS
Molecular weight: 312.3102
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: XAV939 is a small molecule and selective Wnt pathway beta-catenin-mediated transcription inhibitor and axin stabilizing agent with IC50 of 11 and 4 nM for the inhibition of TNKS1 and TNKS2, respectively. IC50 Value: 11 nM(TNKS1), 4 nM(TNKS2) Target: TMKS1/2, beta-catenin in vitro: XAV-939 specifically inhibits tankyrase PARP activity. XAV-939 dramatically decreases DNA-PKcs protein levels, confirming the critical role of tankyrase poly-ADP-ribosylation activity in maintaining stability of the DNA-PKcs protein. The greatest reduction of DNA-PKcs protein levels (< 25% relative expression compared to DMSO treated controls) occurs at 12 hours with 1.0 uM XAV-939 exposure. Treatment of human lymphoblasts with 1.0 uM XAV-939 results in marked elevation of tankyrase 1 levels. XAV-939 is axin stabilizing agent. XAV-939 stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex. XAV-939 stabilizes axin by blocking the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. XAV-939 deregulates the Wnt/b-catenin pathway which has been implicated in many cancers. in vivo: N/A
Safety information: 
MSDS: MSDS
Additional information: 
Synonyms: HY-15147; XAV939; NVP-XAV 939
Gastruloids develop the three body axes in the absence of extraembryonic tissues and spatially localised signalling', Turner D.A. bioRxiv. Jan. 31, 2017. Read more
Wnt/β-catenin signaling participates in the regulation of lipogenesis in the liver of juvenile turbot (Scophthalmus maximus L.)', Liu Dongwu. Comp Biochem Phys B. 2016 Jan;191:155-62. Read more
Soluble (pro)renin receptor via β-catenin enhances urine concentration capability as a target of liver X receptor', Xiaohan Lu. Proc Natl Acad Sci U S A. 2016 Mar 29;113(13):E1898-906. Read more
Epidermal Growth Factor Promotes Proliferation and Migration of Follicular Outer Root Sheath Cells via Wnt/β-Catenin Signaling', Zhang H. Cell Physiol Biochem. 2016;39(1):360-70. Read more
BET bromodomain is a novel regulator of TAZ and its activity.', Duan Q. Biochim Biophys Acta. 2016 Dec;1859(12):1527-1537. Read more
The Neuroprotective Effects of Muscle Derived Stem Cells via Brain Derived Neurotrophic Factor in Spinal Cord Injury Model', Donghe Han. Biomed Res Int. 2017;2017:1972608. Read more
Anteroposterior polarity and elongation in the absence of extraembryonic tissues and spatially localised signalling in Gastruloids, mammalian embryonic organoids', Turner DA. Development. 2017 Nov 1;144(21):3894-3906. Read more
PCDHGA9 acts as a tumor suppressor to induce tumor cell apoptosis and autophagy and inhibit the EMT process in human gastric cancer', Weng J. Cell Death Dis. 2018 Jan 18;9(2):27. Read more