.product-side h2 span {width: 50%;}.product-side h2 span.hover {}Related ProductsArctiinTW-37WEHI-539 hydrochloride2,3-DCPE hydrochlorideMolarity CalculatorDilution Calculator WEHI-539Bcl-xL inhibitor,potent and selectiveCatalog No.A3935SizePriceStockQty5mg$200.00In stock 10mg$245.00In stock 50mg$955.00In stock Tel: +1-832-696-8203Email: sales@apexbt.comWorldwide Distributors Add to CartBulk InquiryFree samples Check OutSample solution is provided at 25 µL, 10mM.Product Citations1. de Jong Y, Monderer D, et al. "Bcl-xl as the most promising Bcl-2 family member in targeted treatment of chondrosarcoma." Oncogenesis. 2018 Sep 21;7(9):74.PMID:302422532. Soderquist RS, Crawford L, et al. "Systematic mapping of BCL-2 gene dependencies in cancer reveals molecular determinants of BH3 mimetic sensitivity." Nat Commun. 2018 Aug 29;9(1):3513.PMID:301585273. Wilson Xuan Mai."Comprehensive Characterization of the Apoptotic Machinery in Glioblastoma Identifies New Therapeutic Strategies." UNIVERSITY OF CALIFORNIA.2018-01-01.4. Dai J, Luftig MA. "Intracellular BH3 Profiling Reveals Shifts in Antiapoptotic Dependency in Human B Cell Maturation and Mitogen-Stimulated Proliferation." J Immunol. 2018 Mar 1;200(5):1727-1736.PMID:293582775. Vuillier C, Lohard S, et al. "E2F1 interacts with BCL-xL and regulates its subcellular localization dynamics to trigger cell death." EMBO Rep. 2017 Dec 12.PMID:292338286. Mai WX, Gosa L, et al. "Cytoplasmic p53 couples oncogene-driven glucose metabolism to apoptosis and is a therapeutic target in glioblastoma." Nat Med. 2017 Nov;23(11):1342-1351.PMID:290353667. Park HA, Licznerski P, et al. "Inhibition of Bcl-xL prevents pro-death actions of ΔN-Bcl-xL at the mitochondrial inner membrane during glutamate excitotoxicity."Cell Death Differ. 2017 Nov;24(11):1963-1974.PMID:287773758. Tan Y, Lin Y, et al. "Selective Antagonism of Bcl-xL Potentiates M1 Oncolysis by Enhancing Mitochondrial Apoptosis." Hum Gene Ther. 2017 Jul 27.PMID:287505649. Rose JC, Stephany JJ, et al. "Rapidly inducible Cas9 and DSB-ddPCR to probe editing kinetics." Nat Methods. 2017 Sep;14(9):891-896.PMID:2873774110. Russo M, Milito A, et al. "CK2 and PI3K are direct molecular targets of quercetin in chronic lymphocytic leukaemia." Oncotarget. 2017 Jun 27;8(26):42571-42587.PMID:2848957211. Bi C, Zhang X, et al."Inhibition of 4EBP phosphorylation mediates the cytotoxic effect of mechanistic target of rapamycin kinase inhibitors in aggressive B-cell lymphomas."Haematologica. 2017 Apr;102(4):755-764.PMID:2810470012. Pécot J, Maillet L, et al. "Tight Sequestration of BH3 Proteins by BCL-xL at Subcellular Membranes Contributes to Apoptotic Resistance." Cell Rep. 2016 Dec 20;17(12):3347-3358.PMID:2800930113. Bennett A, Sloss O, et al. "Inhibition of Bcl-xL sensitizes cells to mitotic blockers, but not mitotic drivers." Open Biol. 2016 Aug;6(8).PMID:2751214114. Kris Cameron Wood,Peter Saville Winter. "Compositions and Methods for Treating Cancer with JAK2 Activity." US Patent App. 15/027,216, 2016.15. Winter PS, et al. "RAS signaling promotes resistance to JAK inhibitors by suppressing BAD-mediated apoptosis." Sci Signal. 2014 Dec 23.PMID:25538080Hide ↑↑Related Compound Libraries DiscoveryProbe™ Bioactive Compound LibraryQuality Control Quality Control & MSDS View current batch: 1 Purity = 99.23% COA (Certificate Of Analysis) HPLC (Retest) NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Chemical structure Related Biological Data Related Biological Data Related Biological Data Related Biological Data Related Biological Data Related Biological Data Related Biological Data Biological ActivityWEHI-539, has high affinity (subnanomolar) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity. WEHI-539 has a high affinity for BCL-XL (IC50 = 1.1 nM). TargetsBCL-XLIC501.1 nMProtocolCell experiment[1]:Cell linesHuman colon cancer cellPreparation methodThe solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.Reaction Conditions1 μM, 24hApplicationsLimiting dilution analysis with CSCs that were pre-treated with ABT-737, ABT-199 or WEHI-539 revealed that ABT-737 and WEHI-539 both were sufficient to decrease clonogenic capacity, whereas ABT-199 did not affect clonogenic growth. As WEHI-539 is selective for BCLXL, this points to a dependency of CSCs on BCLXL for survival. Importantly, ABT-737- or WEHI-539-induced loss of clonogenicity could be restored when BCLXL was ectopically overexpressed. When spheroid cultures were treated with ABT-737 or WEHI-539 compounds, CSCs were effectively sensitized toward oxaliplatin and other chemotherapeutic agents.References:1. Colak S, Zimberlin CD, Fessler E et al. Decreased mitochondrial priming determines chemoresistance of colon cancer stem cells. Cell Death Differ. 2014 Jul;21(7):1170-7.WEHI-539 Dilution CalculatorConcentration (start)xVolume (start)=Concentration (final)xVolume (final) femtomolar picomolar nanomolar micromolar millimolar molar nanoliter microliter milliliter liter femtomolar picomolar nanomolar micromolar millimolar molar microliter milliliter liter C1V1C2V2calculateWEHI-539 Molarity CalculatorMass=ConcentrationxVolumexMW* picograms nanograms micrograms milligrams grams kilograms femtomolar picomolar nanomolar micromolar millimolar molar nanoliter microliter milliliter liter g/molcalculate Chemical Properties Cas No. 1431866-33-9SDF Download SDF Synonyms WEHI539,WEHI 539 Chemical Name 5-[3-[4-(aminomethyl)phenoxy]propyl]-2-[(8E)-8-(1,3-benzothiazol-2-ylhydrazinylidene)-6,7-dihydro-5H-naphthalen-2-yl]-1,3-thiazole-4-carboxylic acid Canonical SMILES C1CC2=C(C=C(C=C2)C3=NC(=C(S3)CCCOC4=CC=C(C=C4)CN)C(=O)O)C(=NNC5=NC6=CC=CC=C6S5)C1 Formula C31H29N5O3S2 M.Wt 583.72 Solubility Storage Store at -20°CPhysical AppearanceA solidShipping ConditionEvaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon requestGeneral tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. BackgroundWEHI-539 is a small-molecule inhibitor of BCLXLwith an IC50 value of 1.1 nM [1].WEHI-539 was designed as a BCL-XLinhibitor with high affinity. It interacted the with the binding groove of BCL-XLwith a Kd value of 0.6 nM. In MEF cells lacking MCL-1, WEHI-539 induced apoptosis which was evidenced by the release of mitochondrial cytochrome cand caspase-3 processing. In BCL-XLoverexpressed MEF cells, WEHI-539 showed EC50 value of 0.48 μM. WEHI-539 also significantly induced apoptosis of the platelets purified from mice. Besides that, WEHI-539can not kill MEF cells lacking BAK because the cell death mediator BAK is regulated by BCL-XLand MCL-1. [1].References:[1] Lessene G, Czabotar P E, Sleebs B E, et al. Structure-guided design of a selective BCL-XL inhibitor. Nature chemical biology, 2013, 9(6): 390-397.