BV6 |
Catalog No.GC12333
One-Click Copy Product Info
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BV6은 세포자멸사 억제제(IAP) 계열의 구성원인 cIAP1 및 XIAP의 길항제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1001600-56-1
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
MCF-7 cells |
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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. |
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Reaction Conditions |
0, 1, 5, 10, and 20µM; 24h |
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Applications |
BV6 treatment inhibited the cell viability of MCF-7 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Female BALB/c mice |
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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. |
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Dosage form |
10mg/kg for once; i.p. |
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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. |
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References: |
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| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 829.5 μL | 4.1474 mL | 8.2948 mL |
| 5 mM | 165.9 μL | 829.5 μL | 1.659 mL |
| 10 mM | 82.9 μL | 414.7 μL | 829.5 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
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Purity: = 98.27% Appearance: A solid
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
- NMR
- HPLC
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)