BV6 [1001600-56-1]
Cat# B4653-5mg
Size : 5mg
Brand : APExBIO Technology
BV6
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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].
References:
[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.
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- 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
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- 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
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- 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
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Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 1205.57 |
Cas No. | 1001600-56-1 |
Formula | C70H96N10O8 |
Solubility | ≥60.28 mg/mL in DMSO; insoluble in H2O; ≥12.6 mg/mL in EtOH with ultrasonic |
Chemical 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) |
SDF | Download SDF |
Canonical 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= |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Cell experiment [1]: | |
Cell lines | HCC193 and H460 non-small cell lung cancer (NSCLC) cell lines. |
Preparation method | Limited solubility. 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 Conditions | 37°C |
Applications | BV6 reduces the expression of cIAP1 and XIAP in HCC193 and H460 cell lines in a time and dose-dependent manner. BV6 also induces apoptosis in both HCC193 and H460 cell lines. In addition, BV6 prominently promotes the radiosensitivity of both HCC193 and H460 lung cancer cell lines. |
Animal experiment [2]: | |
Animal models | Mouse endometriosis model |
Dosage form | Single i.p. injection of BV6 (10 mg/kg) twice weekly. |
Applications | BV6 treatment for 4 weeks attenuates the intensity of IAPs expression and lowers the total number of lesions, the average weight and the surface area of lesions as compared with control group. Moreover, BV6 treatment decreases the percentage of Ki67-positive cells in the endometrial gland epithelia or stroma. |
Other notes | Please 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. Li W, Li B, Giacalone NJ, Torossian A et al. BV6, an IAP antagonist, activates apoptosis and enhances radiosensitization of non-small cell lung carcinoma in vitro. J Thorac Oncol. 2011 Nov;6(11):1801-9. 2. Uegaki T, Taniguchi F, Nakamura K et al. Inhibitor of apoptosis proteins (IAPs) may be effective therapeutic targets for treating endometriosis. Hum Reprod. 2015 Jan;30(1):149-58. |
Description | BV6, a small-molecule Smac mimetic, is an antagonist of IAP proteins. | |||||
Targets | ||||||
IC50 |