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ApexBio/HA14-1/10mM (in 1mL DMSO)/A8168

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.product-side h2 span {width: 50%;}.product-side h2 span.hover {}Related ProductsABT-199SabutoclaxTW-37ABT-737WEHI-539 hydrochlorideObatoclax mesylate (GX15-070)Molarity CalculatorDilution Calculator HA14-1Bcl-2 inhibitor,potent and cell-permeableCatalog No.A8168SizePriceStockQty10mM (in 1mL DMSO)$55.00In stock 20mg$50.00In stock 50mg$110.00In stock 200mg$260.00In stock Tel: +1-832-696-8203Email: sales@apexbt.comWorldwide Distributors Add to CartBulk InquiryFree samples Check OutSample solution is provided at 25 µL, 10mM.Publications citing ApexBio ProductsNature.2017 Jan 19;541(7637):417-420.Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Related Compound Libraries DiscoveryProbe™ Bioactive Compound LibraryDiscoveryProbe™ Anti-cancer Compound LibraryDiscoveryProbe™ Apoptosis Compound LibraryQuality Control Quality Control & MSDS View current batch: 21 Purity = 95.11% COA (Certificate Of Analysis) HPLCMS (Mass Spectrometry) NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Purity = 98.79% COA (Certificate Of Analysis) HPLC NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Chemical structure Biological ActivityHA14-1 is a non-peptidic ligand of a Bcl-2 surface pocket with IC50 of 9 μMTargetsBcl-2IC509 μMProtocolCell experiment [1-3]:Cell linesHL-60 cells, follicular lymphoma B cell lines, HF1A3, HF4.9 and HF28RA cellsPreparation methodThe solubility of this compound in DMSO is >20.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.Reacting condition50 μM, 4 hApplicationsIn HL-60 cells, HA14-1 induced cell death in a dose-dependent manner. HA14-1 (50 μM) caused the loss of viability in more than 90% of the cells. In HL-60 cells, treatment with 50 μM HA14-1 by 3 h displayed the characteristic pattern of DNA fragmentation. HA14-1 decreased cell viability and induced apoptosis in follicular lymphoma B cell lines, HF1A3, HF4.9 and HF28RA cells. HA14-1 (10-20 μmol/L) increased sensitivity of human glioblastoma cells to radiotherapy-induced apoptosis and chemotherapy-induced apoptosis.Animal experiment [3]:Animal modelsSwiss nude mice challenged with BeGBM cellsDosage formIntraperitoneal injection, 400 nM, once weekly from day 2ApplicationIn Swiss nude mice challenged with BeGBM cells, HA14-1 (400 nmol, once weekly from day 2) did not have any significant effect on the growth of glioblastoma tumors in immunodeficient mice. HA14-1 (400 nM) increased the effect of the DNA-damaging agent etoposide (2.5 mg/kg) on glioblastoma growth in vivo.Other notesPlease test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.References:[1]. Wang J L, Liu D, Zhang Z J, et al. Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells[J]. Proceedings of the National Academy of Sciences, 2000, 97(13): 7124-7129.[2]. Skommer J, Wlodkowic D, Mtt M, et al. HA14-1, a small molecule Bcl-2 antagonist, induces apoptosis and modulates action of selected anticancer drugs in follicular lymphoma B cells[J]. Leukemia research, 2006, 30(3): 322-331.[3]. Manero F, Gautier F, Gallenne T, et al. The small organic compound HA14-1 prevents Bcl-2 interaction with Bax to sensitize malignant glioma cells to induction of cell death[J]. Cancer research, 2006, 66(5): 2757-2764.HA14-1 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 C1V1C2V2calculateHA14-1 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. 65673-63-4SDF Download SDF Chemical Name ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate Canonical SMILES CCOC(=O)C1=C(OC2=C(C1C(C#N)C(=O)OCC)C=C(C=C2)Br)N Formula C17H17BrN2O5 M.Wt 409.23 Solubility ≥20.45mg/mL in DMSO Storage Desiccate 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. BackgroundHA14-1 is a potent small-molecule inhibitor of B-cell lymphoma 2 (Bcl-2), a protein factor binding to and inactivating pro-apoptotic proteins (such as Bax and BH3-only family proteins) to suppress apoptosis, that potently inhibits the anti-apoptotic of Bcl-2 and induces apoptosis with values of 50% inhibition concentration IC50 ranging from 10 to 20 μM in NIH3T3, HL60 and lung cancer H1299 cell lines. HA14-1 binds to Bcl-2 by mimicking the BH3 domain required for homo- and hetero-dimer formation and hence prevents the binding of these proteins subsequently resulting in the inhibition of Bcl-2. HA14-1 has been widely investigated in studies of apoptosis, which potentiates it to be used for the treatment of cancer.ReferenceChen J, Freeman A, Liu J, Dai Q, Lee RM. The apoptotic effect of HA14-1, a Bcl-2-interacting small molecular compound, requires Bax translocation and is enhanced by PK11195. Mol Cancer Ther. 2002 Oct;1(12):961-7.Niino S, Nakamura Y, Hirabayashi Y, Nagano-Ito M, Ichikawa S. A small molecule inhibitor of Bcl-2, HA14-1, also inhibits ceramide glucosyltransferase. Biochem Biophys Res Commun. 2013 Apr 5;433(2):170-4. doi: 10.1016/j.bbrc.2013.02.052. Epub 2013 Feb 26.

APExBIO（APExBIO Technology LLC）总部位于美国休斯顿，是一家自主研发生产、致力于为生命科学研究提供高性能产品和优质服务的供应商。公司现阶段涵盖丰富的产品线，主要包括：1. 10000 多种小分子抑制剂/激动剂——用于肿瘤、免疫、神经等生物医药各研究领域。2. 40 余个高通量化合物库——药物筛选最佳工具。3. 分子生物学产品——PCR、逆转录、qPCR、克隆、高通量 DNA 文库构建等试剂和试剂盒，公司对相关酶进行改造，使其稳定性、催化活性等有极大的提升。4. 体外转录——公司拥有国内独家mRNA体外转录合成平台，提供优质的修饰核苷酸、转录酶等各种合成原料，并可提供mRNA订制服务。5. Cy 染料、生物素——高纯度、种类丰富的 Cy 染料和生物素可用于蛋白检测、纯化等研究。6. 免疫学产品——各类细胞器染料及靶标信号放大的链霉亲和素系列和TSA系列。7. 试剂盒——高性能的 MTT、CCK-8、EdU 细胞增殖与毒性检测 Kit 和 Annexin V、Caspase 凋亡检测 Kit。8. 蛋白研究——蛋白提取抑制剂 cocktail、磷酸化蛋白研究新工具 phosbind。9. 组学服务——提供微生物多样性、转录组学等高通量测序服务。