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规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1mL(10 mM in DMSO) | ¥2636.00 | 现货 | |
5mg | ¥954.00 | 现货 | |
25mg | ¥3090.00 | 现货 | |
100mg | ¥6363.00 | 现货 |
特色产品
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- 使用5-moUTP和Cy5-utp修饰
产品描述
BV6是一种选择性的IAP家族抑制剂,在H460细胞中的IC50值为7.2 μM [1]。
IAP(凋亡抑制子)是由8个成员组成的蛋白家族,作为程序性细胞死亡的内源性抑制子。截至目前,已发现5个以上的人IAPs,包括XIAP、c-IAP1、c-IAP-2、NAIP、Livin和Survivin。据报道,IAPs的过表达可以保护细胞抵抗促凋亡刺激,表明IAPs在促进癌细胞存活方面具有至关重要的作用 [2, 3]。
BV6是IAP家族的抑制剂,通常用作佐剂,增加癌细胞对放疗或化疗的敏感性。在H460 非小细胞肺癌(NSCLC)细胞中,BV6预处理增加细胞对放疗的敏感性,通过减少cIAP1和XIAP的表达,以时间和剂量依赖的方式增加细胞凋亡。在白血病THP-1细胞中,BV6预处理增加CIK细胞的杀伤能力,在实体恶性肿瘤RH30细胞中也得到了同样的结果 [4]。
在从供体小鼠子宫组织获得移植腹腔的BALB / c小鼠模型中,腹腔注射BV6通过抑制IAPs的表达,从而抑制子宫内膜异位症的发展和细胞增殖活性 [5]。
参考文献:
[1]. Li, W., et al., BV6, an IAP antagonist, activates apoptosis and enhances radiosensitization of non-small cell lung carcinoma in vitro. J Thorac Oncol, 2011. 6(11): p. 1801-9.
[2]. Altieri, D.C., Survivin - The inconvenient IAP. Semin Cell Dev Biol, 2015.
[3]. Fulda, S., Smac mimetics as IAP antagonists. Semin Cell Dev Biol, 2014.
[4]. Rettinger, E., et al., SMAC Mimetic BV6 Enables Sensitization of Resistant Tumor Cells but also Affects Cytokine-Induced Killer (CIK) Cells: A Potential Challenge for Combination Therapy. Front Pediatr, 2014. 2: p. 75.
[5]. Uegaki, T., et al., Inhibitor of apoptosis proteins (IAPs) may be effective therapeutic targets for treating endometriosis. Hum Reprod, 2015. 30(1): p. 149-58.
产品性质
物理外观 | A solid |
CAS号 | 1001600-56-1 |
分子式 | C70H96N10O8 |
分子量 | 1205.57 |
化学名称 | (S,S,2S,2'S)-N,N'-((2S,2'S)-(hexane-1,6-diylbis(azanediyl))bis(3-oxo-1,1-diphenylpropane-3,2-diyl))bis(1-((S)-2-cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)pyrrolidine-2-carboxamide) |
溶解度 | ≥60.28 mg/mL in DMSO; insoluble in H2O; ≥12.6 mg/mL in EtOH with ultrasonic |
SMILES | O=C(CCCCCCCNC([C@@H](NC([C@H]1N(C([C@H](C2CCCCC2)NC([C@H](C)NC)=O)=O)CCC1)=O)CO=C(NCCCCCCNC([C@@H](NC([C@H]1N(C([C@H](C2CCCCC2)NC([C@H](C)NC)=O)=O)CCC1)=O)C(C3=CC=CC=C3)C4=CC=CC=C4)=O)[C@@H](NC([C@H]5N(C([C@H](C6CCCCC6)NC([C@H](C)NC)=O)=O)CCC5)=O)C(C7=CC= |
存储条件 | -20°C |
运输条件 | 蓝冰 |
SDF文件 | Download SDF |
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 | BV6(小分子Smac模拟物)是IAP蛋白的拮抗剂。 |
生物相关数据
质量控制
操作说明
产品引用文献
- 1. Sang-Bing Ong, et al. "Downregulation of Mitochondrial Fusion Protein Expression Affords Protection from Canonical Necroptosis in H9c2 Cardiomyoblasts." Int J Mol Sci. 2024 Mar 2;25(5):2905. PMID: 38474152
- 2. Yugo Fujita, Toshiyuki Yano, et al. "Enhanced nuclear localization of phosphorylated MLKL predicts adverse events in patients with dilated cardiomyopathy." ESC Heart Fail. 2022 Oct;9(5):3435-3451. PMID: 35851586
- 3. Shin Murai, Kanako Takakura, et al. "A FRET biosensor, SMART, monitors necroptosis in renal tubular epithelial cells in a cisplatin-induced kidney injury model." Research Square. December 5th, 2022.
- 4. Manami Semba, Shinji Takamatsu, et al. "Proscillaridin A Sensitizes Human Colon Cancer Cells to TRAIL-Induced Cell Death." Int J Mol Sci. 2022 Jun 23;23(13):6973. PMID: 35805980
- 5. András N Spaan, Anna-Lena Neehus, et al. "Human OTULIN haploinsufficiency impairs cell-intrinsic immunity to staphylococcal α-toxin." Science. 2022 Jun 17;376(6599):eabm6380. PMID: 35587511
- 6. Cliff J. Luke, Stephanie Markovina, et al. "Lysoptosis is an evolutionarily conserved cell death pathway moderated by intracellular serpins." Commun Biol. 2022 Jan 12;5(1):47. PMID: 35022507
- 7. Tae-Yeon Kim, Ju-Hui Kang, et al. "Down-regulation of pro-necroptotic molecules blunts necroptosis during myogenesis." Biochem Biophys Res Commun. 2021 Jun 11;557:33-39. PMID: 33862457
- 8. Miles MA, Caruso S, et al. "Smac mimetics can provoke lytic cell death that is neither apoptotic nor necroptotic." Apoptosis. 2020;10.1007/s10495-020-01610-8. PMID: 32440848
- 9. Miyake S, Murai S, et al. "Identification of the hallmarks of necroptosis and ferroptosis by transmission electron microscopy." Biochem Biophys Res Commun. 2020;527(3):839-844. PMID: 32430176
- 10. Lei W, Duan R, et al. "The IAP Antagonist SM-164 Eliminates Triple-Negative Breast Cancer Metastasis to Bone and Lung in Mice." Sci Rep. 2020;10(1):7004. PMID: 32332865
- 11. Abe K, Yano T, et al. "mTORC1 inhibition attenuates necroptosis through RIP1 inhibition-mediated TFEB activation." Biochim Biophys Acta Mol Basis Dis. 2019 Sep 6:165552. PMID: 31499159
- 12. Liu Z, Mar KB, et al. "A NIK-SIX signalling axis controls inflammation by targeted silencing of non-canonical NF-κB." Nature. 2019 Apr;568(7751):249-253. PMID: 30894749
- 13. Rossi A, Pakhomova ON, et al. "Mechanisms and immunogenicity of nsPEF-induced cell death in B16F10 melanoma tumors." Sci Rep. 2019 Jan 23;9(1):431. PMID: 30674926
- 14. In EJ, Lee Y, et al. "Identification and Characterization of NTB451 as a Potential Inhibitor of Necroptosis." Molecules.2018 Nov 5;23(11). pii: E2884. PMID: 30400632
- 15. Murai S, Yamaguchi Y, et al. "A FRET biosensor for necroptosis uncovers two different modes of the release of DAMPs." Nat Commun. 2018 Oct 26;9(1):4457. PMID: 30367066
- 16. Yue Y, Nabar NR, et al. "SARS-Coronavirus Open Reading Frame-3a drives multimodal necrotic cell death." Cell Death Dis. 2018 Sep 5;9(9):904. PMID: 30185776
- 17. Dionísio PEA, Oliveira SR, et al. "Loss of Microglial Parkin Inhibits Necroptosis and Contributes to Neuroinflammation." Mol Neurobiol. 2018 Aug 3. PMID: 30074231
- 18. Hao Q, Tang H. "Interferon-γ and Smac mimetics synergize to induce apoptosis of lung cancer cells in a TNFα-independent manner." Cancer Cell Int. 2018 Jun 14;18:84. PMID: 29946223
- 19. Borghi A, Haegman M, et al. "The E3 ubiquitin ligases HOIP and cIAP1 are recruited to the TNFR2 signaling complex and mediate TNFR2-induced canonical NF-κB signaling." Biochem Pharmacol. 2018 Jan 31. pii: S0006-2952(18)30039-X. PMID: 29378181
- 20. Welters MJP, Ma W, et al. "Intratumoral HPV16-Specific T Cells Constitute a Type I-Oriented Tumor Microenvironment to Improve Survival in HPV16-Driven Oropharyngeal Cancer." Clin Cancer Res. 2018 Feb 1;24(3):634-647. PMID: 29018052
- 21. Panayotopoulou EG, Müller AK, et al. "Targeting of apoptotic pathways by SMAC or BH3 mimetics distinctly sensitizes paclitaxel-resistant triple negative breast cancer cells."Oncotarget. 2017 Jul 11;8(28):45088-45104. PMID: 28187446
- 22. Shekhar TM, Miles MA, et al."IAP antagonists sensitize murine osteosarcoma cells to killing by TNFα."Oncotarget. 2016 Jun 7;7(23):33866-86. PMID: 27129149