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BV6

Catalog No.GC12333

Selective inhibitor of IAP proteins

Products are for research use only. Not for human use. We do not sell to patients.

BV6 Chemical Structure

Cas No.: 1001600-56-1

Size Price Stock Qty
10mM (in 1mL DMSO)
$196.00
In stock
5mg
$72.00
In stock
25mg
$241.00
In stock
100mg
$471.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

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 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

37℃

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.

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].
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.

Chemical Properties

Cas No. 1001600-56-1 SDF
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)
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=
Formula C70H96N10O8 M.Wt 1205.57
Solubility ≥ 60.2785mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 0.8295 mL 4.1474 mL 8.2948 mL
5 mM 0.1659 mL 0.8295 mL 1.659 mL
10 mM 0.0829 mL 0.4147 mL 0.8295 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 39 reference(s) in Google Scholar.)

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