XAV939: sc-296704. Western blot analysis of Tankyrase-1/2 expression in untreated (A) and XAV939 treated (B) SW480 whole cell lysates. Note upregulation of Tankyrase-1/2 expression in lane B. Antibody tested: Tankyrase-1/2 (H-350): sc-8337.
XAV939 (CAS 284028-89-3)
See product citations (26)
Alternate Names:
3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one
Application:
XAV939 is a potent inhibitor of beta-catenin, TNKS1, and TNKS2
CAS Number:
284028-89-3
Purity:
≥98%
Molecular Weight:
312.31
Molecular Formula:
C14H11F3N2OS
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
XAV939 is a potent, small molecule inhibitor of tankyrase 1 (TNKS) (IC50 = 11 nM) and tankyrase 2 (IC50 = 4 nM). By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of beta-catenin in SW480 cells. At concentrations as low as 0.3 muM, XAV939 inhibits colony formation of APC-deficient colorectal cancer cells.
XAV939 (CAS 284028-89-3) References
- Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. | Huang, SM., et al. 2009. Nature. 461: 614-20. PMID: 19759537
- XAV939, a small molecular inhibitor, provides neuroprotective effects on oligodentrocytes. | Chen, J., et al. 2014. J Neurosci Res. 92: 1252-8. PMID: 24861203
- XAV939 promotes apoptosis in a neuroblastoma cell line via telomere shortening. | Tian, X., et al. 2014. Oncol Rep. 32: 1999-2006. PMID: 25190315
- XAV939-mediated ARTD activity inhibition in human MB cell lines. | Renna, C., et al. 2015. PLoS One. 10: e0124149. PMID: 25835728
- XAV939 Inhibits Intima Formation by Decreasing Vascular Smooth Muscle Cell Proliferation and Migration Through Blocking Wnt Signaling. | Chen, L., et al. 2016. J Cardiovasc Pharmacol. 68: 414-424. PMID: 27525574
- Multi‑layered prevention and treatment of chronic inflammation, organ fibrosis and cancer associated with canonical WNT/β‑catenin signaling activation (Review). | Katoh, M. 2018. Int J Mol Med. 42: 713-725. PMID: 29786110
- XAV939 inhibits the proliferation and migration of lung adenocarcinoma A549 cells through the WNT pathway. | Li, C., et al. 2018. Oncol Lett. 15: 8973-8982. PMID: 29805633
- XAV939, a Wnt/β-catenin pathway modulator, has inhibitory effects on LPS-induced inflammatory response. | Jang, J., et al. 2019. Immunopharmacol Immunotoxicol. 41: 394-402. PMID: 30466341
- Low Dose of Paclitaxel Combined with XAV939 Attenuates Metastasis, Angiogenesis and Growth in Breast Cancer by Suppressing Wnt Signaling. | Shetti, D., et al. 2019. Cells. 8: PMID: 31416135
- Activation of endothelial Wnt/β-catenin signaling by protective astrocytes repairs BBB damage in ischemic stroke. | Song, S., et al. 2021. Prog Neurobiol. 199: 101963. PMID: 33249091
- Bioactivity Studies of Hesperidin and XAV939. | Fazary, AE., et al. 2021. ACS Omega. 6: 20042-20052. PMID: 34368589
- Ocular Wnt/β-Catenin Pathway Inhibitor XAV939-Loaded Liposomes for Treating Alkali-Burned Corneal Wound and Neovascularization. | Zhong, Y., et al. 2021. Front Bioeng Biotechnol. 9: 753879. PMID: 34765592
- Tankyrase, a poly(ADP-ribose) polymerase at human telomeres. | Smith, S., et al. 1998. Science. 282: 1484-7. PMID: 9822378
Inhibitor of:
β-catenin, β-defensin 27, β-defensin 37, β-defensin 38, β-defensin 39, β-TrCP, δ-catenin, 2410012M07Rik, 2610208M17Rik, 4930451C15Rik, 4930558K02Rik, 4931429I11Rik, 4932411E22Rik, 4932441B19Rik, 4933403O03Rik, 6330503C03Rik, 9430069J07Rik, ALX1, ANKRD37, ANKRD38, ANKRD43, APC, APCDD1, ARMC5, ARMC7, Axin, Barx2, Bcl-9, Bcl-9L, BHLHA9, BICC1, BR-cadherin, brachyury 2, BVES, BY080835, C15orf23, C17orf69, C1orf115, C1orf80, C20orf141, C20orf26, C230072F16Rik, C230099D08Rik, C330013F16Rik, C78339, C86695, Cadherin (CDH), cadherin-24, cadherin-26, cadherin-7, CASPR2, Caspr5-2, CASZ1, CCBE1, CCDC110, CCDC144NL, CCDC36, CD9P-1, CDH20, Cdhr4, CELSR2, CELSR3, Chibby 3, Chox10, claudin-6, CNTNAP3B, Crumbs, CTNNAL1, CTNNBL1, CXXC5, CYYR1, D830046C22Rik, DAAM1, DAPLE, Dapper1, Dapper2, Dapper3, DIXDC1, Dkk-4, DLK2, Dlx-5, Dmp1, DMRTA1, E130311K13Rik, EAP1, ECRG4, EG229879, EG236663, EG245190, EG330689, EG435927, EG436336, EG623459, EMX (Empty Spiracles Homeobox), ERF, Esp4, F-Spondin, FAM123A, FAM124A, FAM46B, FAM90A12, FHL-2, FJX1, FLJ13231, FLJ31818, FLJ45513, FLRT2, Fmi2, FOXD2, FOXD4, frizzled-8, GABP-β2, GATA-5, GBX2, Gcap14, GLTSCR1, Gm12, Gm281, GPR177, H60a, Hairless, HAS1, HB9, HEB, HEF1, HES1, HES3, HOS, HoxC8, HoxD1, HR, ICAT, IQCK, IRF-5, IRX6, ITF-1, K-cadherin, K12, Kremen-2, LEF-1, Lefty, LEKR1_Lekr1, LGI4, LGICZ1, LGR5, LGR6, LHX5, LHX9, LIN-39, LIN-44, LMBR1L, LMX1A, LNX2, LOC100040885, LOC100041243, LOC100041336, LOC100041430, LOC130951, LOC150356, LOC257407, LOC388210, LOC388963, LOC666145, LOC729454, LRP4, LRP5L, LRP6, LRRC27, LRRC29, LRRC44, LRRFIP1, LRRFIP2, Lubricin, Lunatic Fringe, Ly-6C2, MAB-5, MATH-2, MATH-3, MDFIC, Mec1, MESP1, MINK1, MIXL1, mPRβ, Myotubularin (MTM, MTMR), NKD1, Nkx-2.2, Nlk, NMNAT-2, Notum, NYD-SP17, Oct-6, Olfr1051, Olfr482, Olfr697, Olfr698, Olfr699, Olfr700, Olfr908, Olfr974, Olfr975, OLIG3, Olr22, Olr270, OSR2, otoancorin, OTP, p120, PARD3B, PARP L, PARP S, PARP-8, PC-LKC, PCDH11X, PCDH18_Pcdh18, PCDH20_Pcdh20, PCDHA11, PCDHA4, PCDHAC1_Pcdhac1, PCDHB1, Pcdhb19, PCDHB2, PCDHB4, PCDHB5, PCDHGA3, PCDHGB1, PDZK11, Pecanex 1, Pecanex 2, Pitx1, POP-1, POPX1, POU3F, POU3F4, Prickle1, Prickle2, Prickle4, Protein S, PTF1, Pygopus 1, Pygopus 2, R-Spondin2, R-Spondin4, Rad GTPase, RbAp48, Reelin, REG IIIα, RFX4, RGL2, RGPD, rhophilin, Rhox8, RNF146, robo1, RTDR1, SAMD10, Scratch1, SCUBE1, SDAD1, SEMA3E, SEMA5B, SETD3, Shelterin complex, SHISA3, SHKBP1, Sidekick-2, Six3, SKT, Soggy-1, SOSTDC1, Sox-12, SOXN, SP140, Sp6, SPATA19, Spondin (SPON), SRRT (Serrate), T1-cadherin, Tankyrase, Tankyrase-1, Tankyrase-2, TBL1XR1, TBX10, TBX20, TBX5, Tcam1, TCF-1, TCF-19, TCF-3, TCF23, Testican-2, TIEG1, TLE1, TLE2, TLE4, TMEM170B, TMEM191C, TMEM245, TMEM46, TMEM88, TMEM9, TNIK, TRB-1, Trefoil factor (TFF), TRIM54, TTC30B, TTC9, UNCX, USP17L7, USP17L8, V1RC27, Vangl1, VAX2, Vmn1r113, Vmn2r102, WAPL, WBP2, WDPCP, WDR27, WDR42B, WDR5, WIF-1, WISP-1, WISP-3, Wnt-1, Wnt-14b, Wnt-15, Wnt-2, Wnt-3, Wnt-3a, Wnt-5b, Wnt-6, Wnt-7a, WTIP, WTX, XTP13, ZCCHC13, Zfp866, Zic3, ZNF512, ZNF726, ZNF883, ZNRF3, and ZO-3.Activator of:
ADAMTS, ADAMTS-18, ADAMTS-19, AIDA, APC11, APC5, ARHGAP39, Armadillo (β-catenin), BAR-1, BBP, BET3L, BJ-TSA-9, BLOS1, BTNL8, C14orf108, C1orf80, CECR2, CELSR1, Chibby, Ciao 1, Conductin, Crumbs, CUEDC1, cystatin 12, cystatin 13, D230039L06Rik, Dkk-4, DLN1, Dynein Light Chain, Dynlt3, E230028L10Rik, EG245190, FAM13C1, FAM20A, Flamingo, Formin 1, FOXC1, fringe, frizzled-1, frizzled-2, frizzled-3, frizzled-5, frizzled-9, FRNK, FSD1, glypican-6, Gm6772, IFT122, INTU, JAZF1, KCTD11, Kremen-1, Kremen-2, LGR4, LHX2, LIN-31, LIN-41, LIN-44, LRF, Manic Fringe, MOM-4, Nanog, Nek7, nephrocystin, neuropilin, NP1, nudel, OC-3, Olfr394, PARG, PCDHA9, PDE8A, PGBD1, R-Spondin, Rab 3 GAP p130, Rab L2A, Rad23B, RASAL3, RNF43, RYK, Sec31, Six2, Sox-7, Sp5, SUGT1, TCF-4, Testican-1, TIFAB, TMEM170B, TPR, TTC3, Wingless, Wnt-10b, Wnt-11, Wnt-14, Wnt-16, Wnt-2b, Wnt-5a, Wnt-8b, WRM-1, and ZMYM3.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
XAV939, 1 mg | sc-296704 | 1 mg | $36.00 | |||
XAV939, 5 mg | sc-296704A | 5 mg | $117.00 | |||
XAV939, 50 mg | sc-296704B | 50 mg | $525.00 |