Name: BV6
Price: 451.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    BV6 is a selective inhibitor of IAP family with IC50 value of 7.2 μM when tested with H460 cells [1].IAP (inhibitor of apoptosis) is a family protein consists of 8 members and serves as endogenous inhibitors of programmed cell death. Until now, more than 5 human IAPs have been discovered includes XIAP, c-IAP1, c-IAP-2, NAIP, Livin and Survivin. It is reported that IAPs overexpression protects cells against a number of proapoptotic stimuli which enables IAPs play a pivotal role in promoting cancer cell survival [2, 3].BV6 is an inhibitor of IAP family and often used as an adjuvant to sensitize the cancer cells to radiotherapy or chemotherapy. When tested with H460 NSCLC cells, pre-treatment BV6 sensitized the cells to radiation and increased the apoptosis in a time- and dose- dependent manner via reducing the expression of cIAP1 and XIAP [1]. In hematological THP-1 cells, pre-treatment with BV6 increased the CIK cells killing ability and the same results were achieved in solid malignancy RH30 cells [4]In BALB/c mice model with transplanted abdominal cavities from donor mouse uterine tissue, intraperitoneally with BV6 repressed the advancement of endometriosis, cell proliferative activity via inhibiting the expression of IAPs [5].
    
    [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.
- Properties
  - Alternative Name
    
    (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)
    
    CAS Number
    
    1001600-56-1
    
    Molecular Formula
    
    C70H96N10O8
    
    Molecular Weight
    
    1205.57
    
    Appearance
    
    A solid
    
    Purity
    
    98.77%
    
    Solubility
    
    ≥60.28 mg/mL in DMSO; insoluble in H2O; ≥12.6 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. 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
    2. 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
    3. 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
    4. 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
    5. 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
    6. 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
    7. 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
    8. 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
    9. 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
    10. 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
    11. 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
    12. 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
    13. Dionísio PEA, Oliveira SR, et al. "Loss of Microglial Parkin Inhibits Necroptosis and Contributes to Neuroinflammation." Mol Neurobiol. 2018 Aug 3. PMID:30074231
    14. 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
    15. 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
    16. 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
    17. 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
    18. 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

BV6

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