BV-6

Name: BV-6
Brand: Selleck Chemicals
SKU: S7597
Rating: 5 (27 reviews)

For research use only.

Catalog No.S7597

27 publications

Molecular Weight(MW): 1205.57

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

Selleck's BV-6 has been cited by 27 publications

Cell Death Differ, 2020, 26

PubMed: 32457484 ( click the link to review the publication )

Cancer Lett, 2020, 1;472:29-39

PubMed: 31838086 ( click the link to review the publication )

Cell Death Dis, 2020, 4;11(5):305

PubMed: 32366830 ( click the link to review the publication )

Int J Mol Sci, 2020, 28;21(9):E3116

PubMed: 32354117 ( click the link to review the publication )

Immunol Cell Biol, 2020, 10.1111/imcb.12376

PubMed: 32654231 ( click the link to review the publication )

PLoS Pathog, 2020, 16(7):e1008473

PubMed: 32649716 ( click the link to review the publication )

PLoS One, 2020, 15(1):e0228015

PubMed: 31999765 ( click the link to review the publication )

Nat Microbiol, 2019, 10.1038/s41564-019-0624-1

PubMed: 31844296 ( click the link to review the publication )

Nat Commun, 2019, 10(1):1729

PubMed: 30988283 ( click the link to review the publication )

Nat Commun, 2019, 10(1):4157

PubMed: 31519887 ( click the link to review the publication )

EMBO Rep, 2019, 20(2)

PubMed: 30498077 ( click the link to review the publication )

Cell Rep, 2019, 26(8):2194-2211.e6

PubMed: 30784599 ( click the link to review the publication )

Int J Cancer, 2019, 10.1002/ijc.32799

PubMed: 31749151 ( click the link to review the publication )

Cell Chem Biol, 2019, 26(3):331-339

PubMed: 30639259 ( click the link to review the publication )

Clin Sci (Lond), 2019, 133(8):919-932

PubMed: 30944150 ( click the link to review the publication )

Cell Death Dis, 2018, 9(9):874

PubMed: 30158588 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(7):1381-1391

PubMed: 29695633 ( click the link to review the publication )

Toxicol Appl Pharmacol, 2018, 344:35-45

PubMed: 29496522 ( click the link to review the publication )

Fish Shellfish Immunol, 2018, 82:573-578

PubMed: 30176336 ( click the link to review the publication )

Commun Biol, 2018, 1:6

PubMed: 30271893 ( click the link to review the publication )

Clin Cancer Res, 2018, 10.1158/1078-0432.CCR-18-1548

PubMed: 30487125 ( click the link to review the publication )

Cell Mol Life Sci, 2017, 74(3):543-554

PubMed: 27592300 ( click the link to review the publication )

FASEB J, 2017, 10.1096/fj.201700141RR

PubMed: 28710114 ( click the link to review the publication )

Cell Chem Biol, 2017, 24(12):1445-1454

PubMed: 29033315 ( click the link to review the publication )
Cell Death Dis, 2017, 8(6):e2904

PubMed: 28661484 ( click the link to review the publication )

Front Immunol, 2016, 7:496

PubMed: 27920775 ( click the link to review the publication )

Oncotarget, 2016, 7(27):41488-41504

PubMed: 27166192 ( click the link to review the publication )

Purity & Quality Control

Choose Selective IAP Inhibitors

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 J Thorac Oncol 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 Cell Death Dis 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 Cell Death Dis 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 Cell Death Dis 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]

- Collapse

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)

References

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 Download BV-6 SDF

Molecular Weight	1205.57
Formula	C₇₀H₉₆N₁₀O₈.xCF₃COOH
CAS No.	1001600-56-1(freebase)
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CC(C(=O)NC(C1CCCCC1)C(=O)N2CCCC2C(=O)NC(C(C3=CC=CC=C3)C4=CC=CC=C4)C(=O)NCCCCCCNC(=O)C(C(C5=CC=CC=C5)C6=CC=CC=C6)NC(=O)C7CCCN7C(=O)C(C8CCCCC8)NC(=O)C(C)NC)NC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

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Calculation results:

Working concentration： mg/ml；

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 DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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The Serial Dilution Calculator Equation

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Computed Result

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C8=C7/X	C8:	LOG(C8):

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BV-6