GLPBio

BV6

Catalog No.: GC12333Purity:= 98.27%
COASDSData SheetHPLCNMR

BV6, a SMAC mimetic, inhibits the inhibitors of apoptosis proteins (IAPs), causing apoptosis.

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BV6
Cas No.: 1001600-56-1
10mM (in 1mL DMSO)In Stock
$134.00
1
1mgIn Stock
$32.00
1
2mgIn Stock
$44.00
1
5mgIn Stock
$59.00
1
10mgIn Stock
$101.00
1
50mgIn Stock
$300.00
1
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Description

BV6, a SMAC mimetic, inhibits the inhibitors of apoptosis proteins (IAPs), causing apoptosis [1]. BV6 can induce degradation of IAPs, including cIAP1 and cIAP2, and sensitize the resistant cancer cell lines to apoptosis induced by the death ligands TNF-α and TRAIL [2]. BV6 has been widely used to inhibit the growth, clonal formation and angiogenesis of various cancer cells [3].

In vitro, BV6 treatment for 24 hours significantly inhibited the viability of MCF7 and MDA-MB-231 cells, with IC50 values of 5.36μM and 3.71μM [4]. Treatment with 10µM BV6 for 24 hours significantly attenuated the pro-inflammatory signaling induced by TNF and CD40L and triggered the maturation of immature monocyte-derived dendritic cells (iDCs)[5]. 2µM BV6 treatment for 48 hours significantly increased the mRNA and protein expression levels of caspase-3 and caspase-9, and decreased the expression level of LC3-II protein in NCI-H23 cells[6].

In vivo, BV6 treatment via a single intraperitoneal injection at a dose of 10mg/kg significantly inhibited the inflammatory state of endometriosis-like lesions in mice within 4 weeks, and reduced the expression of NF-κB p65 and phosphorylated NF-κB p65[7]. A single intraductal injection of 0.1mg dose of BV6 into the gallbladder significantly induced intrahepatic bile duct injury and inflammatory response in mice within 5 days[8].

References:
[1] Li W, Li B, Giacalone N J, et al. BV6, an IAP antagonist, activates apoptosis and enhances radiosensitization of non-small cell lung carcinoma in vitro[J]. Journal of Thoracic Oncology, 2011, 6(11): 1801-1809.
[2] El-Mesery M, Shaker M E, Elgaml A. The SMAC mimetic BV6 induces cell death and sensitizes different cell lines to TNF-α and TRAIL-induced apoptosis[J]. Experimental Biology and Medicine, 2016, 241(18): 2015-2022.
[3] Nikkhoo A, Rostami N, Farhadi S, et al. Codelivery of STAT3 siRNA and BV6 by carboxymethyl dextran trimethyl chitosan nanoparticles suppresses cancer cell progression[J]. International journal of pharmaceutics, 2020, 581: 119236.
[4] Rafat S, Singh P, Pandey K K, et al. SMAC mimetic BV6 Co-treatment downregulates the factors involved in resistance and relapse of cancer: IAPs and autophagy[J]. Biology, 2022, 11(11): 1581.
[5] Müller-Sienerth N, Dietz L, Holtz P, et al. SMAC mimetic BV6 induces cell death in monocytes and maturation of monocyte-derived dendritic cells[J]. PLoS One, 2011, 6(6): e21556.
[6] Beg M M A, Saxena A, Singh V K, et al. Modulatory role of BV6 and chloroquine on the regulation of apoptosis and autophagy in non-small cell lung cancer cells[J]. Journal of Cancer Research and Therapeutics, 2023, 19(Suppl 1): S341-S348.
[7] Taniguchi F, Uegaki T, Nakamura K, et al. Inhibition of IAP (inhibitor of apoptosis) proteins represses inflammatory status via nuclear factor‐kappa B pathway in murine endometriosis lesions[J]. American Journal of Reproductive Immunology, 2018, 79(1): e12780.
[8] Guicciardi M E, Krishnan A, Bronk S F, et al. Biliary tract instillation of a SMAC mimetic induces TRAIL-dependent acute sclerosing cholangitis-like injury in mice[J]. Cell death & disease, 2018, 8(1): e2535-e2535.

Protocol

Cell experiment [1]:

Cell lines

 MCF-7 cells

Preparation Method

 MCF-7 cells were grown in DMEM medium supplemented with 1% penicillin/streptomycin and 10% heat-inactivated fetal bovine serum (FBS) at 37°C in an incubator with 5% CO2. MCF-7 cells at 8×103 cells/well were seeded in 96-well microtiter plates and incubated at 37°C for 24 hours. Different concentrations of BV6 (0, 1, 5, 10, and 20µM) were treated for 24h, and the cell viability was analyzed.

Reaction Conditions

 0, 1, 5, 10, and 20µM; 24h

Applications

 BV6 treatment inhibited the cell viability of MCF-7 cells in a dose-dependent manner.
Animal experiment [2]:

Animal models

 Female BALB/c mice

Preparation Method

 Female BALB/c mice (6 weeks old) were maintained under a 12h light and 12h dark cycle at a temperature of 25°C and humidity of 50%±10%, free with water and an ad libitum diet. All 36 mice included were ovariectomized through a 1cm longitudinal skin incision, then injected subcutaneously with estradiol valerate (E2: 0.5μg/mouse/week) for 6 weeks until the experimental endometriosis induction and kill. 2 weeks after ovariectomy, the uteri of donor mice (n=12) were removed en bloc after euthanasia and cleaned of excess tissue in sterile saline. Each uterus was cut to include the uterine horns in each half with a linear incision longitudinally and minced (approximately 0.5mm in diameter) with dissecting scissors. The ovariectomized recipient mice (n=24) were anesthetized using pentobarbital sodium. A 0.5cm subabdominal midline incision was made. Each recipient received half of the donor uterus (1:2 donor uterus to host ratio) minced and added to 500μl saline, and injected into the peritoneal cavity, and the peritoneum was sutured. The injected uterine tissue weighed approximately 50mg per mouse. For the next 4 weeks, recipient mice were treated with a single intraperitoneal injection of BV6 (10mg/kg). Endometriosis-like lesions were carefully removed and photographed to document in situ images of the lesions by microscope.

Dosage form

 10mg/kg for once; i.p.

Applications

 BV6 treatment repressed the inflammation status of murine endometriosis-like lesions and reduced the expression of NF-κB p65 and phosphorylated NF-κB p65.

References:
[1] Rafat S, Singh P, Pandey K K, et al. SMAC mimetic BV6 Co-treatment downregulates the factors involved in resistance and relapse of cancer: IAPs and autophagy[J]. Biology, 2022, 11(11): 1581.
[2] Taniguchi F, Uegaki T, Nakamura K, et al. Inhibition of IAP (inhibitor of apoptosis) proteins represses inflammatory status via nuclear factor‐kappa B pathway in murine endometriosis lesions[J]. American Journal of Reproductive Immunology, 2018, 79(1): e12780.

Product Documents

Purity:= 98.27%Appearance:A solid
COASDSData SheetHPLCNMR

Chemical Properties

CAS No.
1001600-56-1
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)
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=
Molecular Formula
C70H96N10O8
Molecular Weight
1205.57
Solubility
≥ 60.2785mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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