Catalog No. A3935
WEHI-539
选择性的Bcl-xL抑制剂
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 5mg | ￥1636.00 | 现货 | |
| 10mg | ￥2181.00 | 现货 | |
| 50mg | ￥8181.00 | 现货 |
CAS号：1431866-33-9纯度：95.06%
仅用于科研，不用于诊疗。未经明确授权不得转售。
A
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特色产品
Annexin V-FITC/PI Apoptosis Kit
用于双染检测细胞凋亡和坏死
- 在10-20分钟内完成染色
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
Phos binding reagent (Phosbind) acrylamide
分离和检测磷酸化/非磷酸化蛋白
- 新型的磷酸盐结合标签和功能分子
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
Cell Counting Kit-8 (CCK-8)
用于细胞增殖和细胞毒性试验
- 比MTT，MTS或WST-1更敏感
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
Cy5 TSA Fluorescence System Kit
Cy5荧光标记的酪胺信号放大系统
- 检测ICC/IHC/ISH中的低丰度靶点
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
EZ Cap™ Cy5 Firefly Luciferase mRNA (5-moUTP)
用于观察mRNA运送，定位，翻译
- 具有Cap1结构的荧光素酶mRNA
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
HotStart™ 2X Green qPCR Master Mix
用于荧光定量目标DNA或cDNA
- 通过热启动机制优化扩增特异性
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单
HyperScribe™ T7 High Yield Cy5 RNA Labeling Kit Plus
高效的Cy5修饰RNA转录试剂盒
- 适合原位/Northernblot杂交实验
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量
产品描述
WEHI-539是BCL_x001E_XL的小分子抑制剂，IC50值为1.1 nM [1]。
WEHI-539是一个高亲和性的BCL_x001E_XL抑制剂，与BCL-XL的特定结构域相互作用，Kd值为0.6 nM。在缺乏MCL-1的MEF细胞中，WEHI-539诱导细胞凋亡，证据显示线粒体细胞色素C的释放和caspase-3的加工。在BCL-XL过表达的MEF细胞中，WEHI-539诱导细胞凋亡，EC50值为0.48 μM。
WEHI-539也可以显著诱导从小鼠中纯化的血小板细胞的凋亡。由于促凋亡调节蛋白BAK是由BCL-XL和MCL-1调控的，因此，WEHI-539不能诱导缺乏BAK的MEF细胞的凋亡[1]。
参考文献：
[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.
产品性质
| 物理外观 | A solid |
| CAS号 | 1431866-33-9 |
| 分子式 | C31H29N5O3S2 |
| 分子量 | 583.72 |
| 化学名称 | 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 |
| 溶解度 | insoluble in DMSO; insoluble in H2O; insoluble in EtOH |
| 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 |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)
IC50和靶点
| 生物活性描述 | WEHI-539是一种高亲和性和选择性的BCL-XL抑制剂，IC50值为1.1 nM。WEHI-539通过选择性地拮抗BCL-XL的促生存活性从而有效杀死细胞。 |
| 靶点 | Bcl-xL |
| 生物活性数据 | 1.1 nM |
生物相关数据
质量控制
APExBIO 顾客使用本产品发表的 27 篇科研文献
- 1. Iseghohimen, Adesuwa. "Overcoming drug resistance: targeting the BCL-2 family and the long non-coding RNA HCP5 in medulloblastoma and colorectal cancer." University of Salford Manchester, Jul 3, 2023.
- 2. Venneker, S. "Exploiting vulnerabilities induced by recurrent mutations in chondrosarcoma and giant cell tumour of bone: therapeutic targeting of the altered epigenome and beyond." Leiden University Scholarly Publications. Jan 01, 2023.
- 3. Loo, Larry Sai Weng. "Dynamics of BCL-2 family of proteins in early pancreatic progenitors and β-cells." Nanyang Technological University.
- 4. Boccellato, Chiara, et al. "Overcoming glioblastoma intractability: pre-clinical characterisation of TRAIL sensitisation by marizomib and novel treatment perspectives." Universität Stuttgart. 2022.
- 5. Yasmeen A. Albalawi, Srinivas D. Narasipura, et al. "Wnt/β-Catenin Protects Lymphocytes from HIV-Mediated Apoptosis via Induction of Bcl-xL." Viruses. 2022 Jul 2;14(7):1469. PMID: 35891449
- 6. Nadine Pollak, Aline Lindner, et al. "Cell cycle progression and transmitotic apoptosis resistance promote escape from extrinsic apoptosis." J Cell Sci. 2021 Dec 15;134(24):jcs258966. PMID: 34806752
- 7. Kirsteen J. Campbell, Susan M. Mason, et al. "Breast cancer dependence on MCL-1 is due to its canonical anti-apoptotic function." Cell Death Differ. 2021 Sep;28(9):2589-2600. PMID: 33785871
- 8. Sanne Venneker, Alwine B. Kruisselbrink, et al. "Beyond the influence of idh mutations: Exploring epigenetic vulnerabilities in chondrosarcoma." Cancers (Basel). 2020 Nov 30;12(12):E3589. PMID: 33266275
- 9. Enyuan Shang, Trang T. T. Nguyen, et al. "Epigenetic Targeting of Mcl-1 Is Synthetically Lethal with Bcl-xL/Bcl-2 Inhibition in Model Systems of Glioblastoma." Cancers 2020, 12(8), 2137;1 August 2020. PMID: 32752193
- 10. Meyer L, Verbist KC, et al. "JAK/STAT pathway inhibition sensitizes CD8 T cells to dexamethasone-induced apoptosis in hyperinflammation." Blood. 2020;blood.2020006075. PMID: 32530039
- 11. Loo LSW, Soetedjo AAP, et al. "BCL-xL/BCL2L1 is a critical anti-apoptotic protein that promotes the survival of differentiating pancreatic cells from human pluripotent stem cells." Cell Death Dis. 2020;11(5):378. PMID: 32424151
- 12. Villalobos-Ortiz M, Ryan J, et al. "BH3 profiling discriminates on-target small molecule BH3 mimetics from putative mimetics." Cell Death Differ. 2019 Jul 22. PMID: 31332296
- 13. 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: 30242253
- 14. 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: 30158527
- 15. Wilson Xuan Mai."Comprehensive Characterization of the Apoptotic Machinery in Glioblastoma Identifies New Therapeutic Strategies." UNIVERSITY OF CALIFORNIA.2018-01-01.
- 16. 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: 29358277
- 17. 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: 29233828
- 18. 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: 29035366
- 19. 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: 28777375
- 20. 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: 28750564
- 21. 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: 28737741
- 22. 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: 28489572
- 23. 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: 28104700
- 24. 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: 28009301
- 25. 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: 27512141
- 26. Kris Cameron Wood,Peter Saville Winter. "Compositions and Methods for Treating Cancer with JAK2 Activity." US Patent App. 15/027,216, 2016.
- 27. Winter PS, et al. "RAS signaling promotes resistance to JAK inhibitors by suppressing BAD-mediated apoptosis." Sci Signal. 2014 Dec 23. PMID: 25538080
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