BV-6

Catalog No.S7597

BV-6 Chemical Structure

Molecular Weight(MW): 1205.57

BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.

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Cited by 7 Publications

2 Customer Reviews

  • IEC-1 cells were transfected with Per1/2 specific siRNAs or a control siRNA. Afterward, the cells were stimulated with TNFa (0.1 ng/ml under basal conditions) in the presence or absence of BV-6 or were left untreated. Activation of caspase-8 (I) and caspases 3/7 (J ) was assayed. Data are presented as the means±SEM of at least 3 independent experiments. *P≤0.05, **P≤0.01.

    FASEB J, 2017, 31(11):4707-4719. BV-6 purchased from Selleck.

    Treatment of primary CLL cells with the SMAC mimetic BV-6 for 2 hours in presence or absence of 200 ng/mL rhBAFF. Immunoblotting was performed in (H) cytoplasmic and (I) nuclear fractions.

    Clin Cancer Res, 2018, doi:10.1158/1078-0432.CCR-18-1548. BV-6 purchased from Selleck.

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Biological Activity

Description BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.
Targets
cIAP [1] XIAP [1]
In vitro

BV6 inhibits the cell viability of HCC193 NSCLC cells with IC50 of 7.2 μM, induces apoptosis in both HCC193 and H460 cell lines, and also significantly enhances the radiosensitivity of these cell lines through activation of cleaved caspase-8 and cleaved caspase-9, respectively. [1] In immature dendritic cells, BV-6 treatment results in moderate activation of the classical NF-kB pathway. [2] Furthermore, BV-6 increases CIK cell-mediated lysis of hematological (H9, THP-1, and Tanoue) and solid malignancies (RH1, RH30, and TE671). BV-6 also enhances apoptosis of peripheral blood mononuclear cells and most notably has an inhibitory effect on immune cells limiting their cytotoxic potential. [3]
Assay
Methods Test Index PMID
Western blot
cIAP1 / XIAP ; 

PubMed: 21760551     


Cells were treated with DMSO (control) or BV6 (1μM for HCC193 and 5μM for H460) and harvested at indicated time points. BV6 reduced cIAP1 within one hour and gradually decreased XIAP with increased incubation time for both cell lines. 

RIP1 / FADD / Caspase-8; 

PubMed: 24287697     


A172 cells were treated for indicated times with 5 μM BV6 in the presence of 20 μM zVAD.fmk. Caspase-8 was immunoprecipitated using an anti-caspase-8 antibody and detection of indicated proteins was done by western blotting. 

p52 / RelB / p50 / p-p65 / Lamin B1; 

PubMed: 24287697     


A172 and MDA-MB-231 cells were treated for indicated times with 5 μM BV6 (A172) or 50 nM BV6 (MDA-MB-231). Expression levels of p50, p52, p65 and RelB were analyzed in the nucleus or in the cytosol by western blotting. α-tubulin served as purity control for cytoplasmic fractions, lamin B1 for nuclear fractions and β-actin as loading control for both fractions. 

21760551 24287697
Growth inhibition assay
Cell death ; 

PubMed: 26775704     


Intrinsic activity of BV6 on BCP-ALL cell lines. (a) Heterogeneous sensitivity of BCP-ALL cell lines for cell death after exposure to BV6 (48 h). UoCB6 and REH display half-maximal inhibitory concentration (IC50) values at nanomolar concentrations in contrast to Nalm-6 and RS4;11 showing sensitivity in the micromolar range. (b–e) Inhibition of BV6-induced cell death (48-h exposure to BV6 at indicated concentrations) by 20 μM zVAD.fmk (zVAD), 30 μM Necrostatin-1 (Nec-1), or 40 μg/ml etanercept (Et). Percentages of dead cells were estimated by flow cytometry according to forward and side scatter criteria, three independent experiments each performed in triplicate, estimation of IC50 (a), comparison of BV6 to BV6 and the respective inhibitors; mean and S.D. are indicated; significance by Mann-Whitney U-test; *P<0.01 and #P<0.05 (b-e)

26775704

Protocol

Cell Research:[1]
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  • Cell lines: HCC193 and H460 cells
  • Concentrations: ~30 μM
  • Incubation Time: ~48 hours
  • Method: Cell viability is measured using the CellTiter 96® Aqueous Non-Radioactive Cell Proliferation Assay kit. 5000 cells/well are seeded into 96-well plates in triplicate. Following adhesion of cells to the wells, increasing concentrations of BV6 are added into different wells. Control groups are exposed to the same concentration of DMSO. The final concentrations of 333 μg/mL MTS and 25 μM PMS are added to each well 24 hours later. After two hours incubation at 37 °C in humidified 5% CO2, plates are read at the absorbance of 490-nm on a microplate reader. Relative cell viability of an individual sample is calculated by normalizing their absorbance to that of the corresponding control. IC50 values are calculated using Prism 5.01. For the TNFα neutralizing antibody assay, cells are exposed to 1 and 5 μM BV6 with or without 10 μg/mL infliximab and the assay is performed 24 hours later. Plates are read at the absorbance of 490-nm on a microplate reader
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (82.94 mM)
Ethanol 100 mg/mL warmed (82.94 mM)
Water 25 mg/mL (20.73 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 1205.57
Formula

C70H96N10O8.xCF3COOH
CAS No. 1001600-56-1(free base)
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID