Bax inhibitor peptide V5
(Synonyms: BIP-V5; BAX Inhibiting Peptide V5) 目录号 : GC17195A Bax inhibitor
Cas No.:579492-81-2
Sample solution is provided at 25 µL, 10mM.
Bax inhibitor peptide V5 (BIP V5) is a peptide inhibitor of Bax translocation to mitochondria [1].
Bax is a pro-apoptotic member of Bcl-2 family proteins and plays an important role in mitochondria-dependent apoptosis. Bax stays in the cytosol and transfers into mitochondria after apoptotic stimuli [1].
BIP V5 is a membrane-permeable peptide inhibitor of Bax translocation to mitochondria. In HeLa cells, BIP V5 protected cells from UVC- and STS-induced apoptosis. In U87-MG glioma cells, MCF-7 breast cancer cells and LNCaP prostate cancer cells, BIP V5 also inhibited apoptosis induced by anti-cancer drugs cisplatin, etoposide and doxorubicin. While BIP V5 did not suppress UVC- or STS-induced apoptosis in Bax-deficient cells (DU145), which suggested BIP V5 only suppressed Bax-mediated apoptosis. Also, BIP (V5) inhibited Bax translocation to mitochondria stimulated by UVC irradiation and STS treatment. The caspase activation and the release of cytochrome c from mitochondria triggered by apoptotic stimuli were also significantly inhibited by BIP V5. BIP V5 inhibited the interaction of Ku70 and endogenous Bax in a dose-dependent way [1].
In a mouse model, BIP V5 increased expression of anti-apoptotic proteins XIAP and Bcl-2 by more than 11- and 3-fold and reduced expression of apoptosis-inducing proteins Bax, Bad, and nuclear factor-κ B-p65 by 10, 30, and nearly 50%, respectively. Also, BIP V5 increased glucose-responsive insulin secretion [2].
References:
[1]. Sawada M, Hayes P, Matsuyama S. Cytoprotective membrane-permeable peptides designed from the Bax-binding domain of Ku70. Nat Cell Biol, 2003, 5(4): 352-357.
[2]. Rivas-Carrillo JD, Soto-Gutierrez A, Navarro-Alvarez N, et al. Cell-permeable pentapeptide V5 inhibits apoptosis and enhances insulin secretion, allowing experimental single-donor islet transplantation in mice. Diabetes, 2007, 56(5): 1259-1267.
Cell experiment [1,2]: | |
Cell lines |
Mouse islet isolation |
Preparation method |
The solubility of this compound in DMSO is >24.1mg/mL. 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. |
Reacting condition |
0-100 μM, 24 h |
Applications |
Bax inhibitor peptide V5 (0-50 μM) reduced cell death in STF-cMyc cells but not in SW620 or NCI-H23 cells. BIP V5 does not result in any significant effect on cell cycle arrest at the G2/M phase. In mouse islet isolation, BIP V5 (100 μM) treatment upregulated expression of anti-apoptotic proteins Bcl-2 and XIAP by more than 3- and 11-fold and downregulated expression of apoptosis-inducing proteins Bax, Bad, and nuclear factor-κB-p65 by 10, 30, and nearly 50%, respectively. |
Animal experiment [2]: | |
Animal models |
Streptozotocin-induced diabetic mice |
Dosage form |
100 μmol/l |
Application |
Following transplantation in streptozotocin-induced diabetic mice, 150 BIP V5-treated islet equivalents functioned as well as 450 control untreated islet equivalents in normalizing blood glucose. |
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]. Jo M J, Paek A R, Choi J S, et al. Regulation of cancer cell death by a novel compound, C604, in a c-Myc-overexpressing cellular environment[J]. European journal of pharmacology, 2015, 769: 257-265. [2]. Sawada M, Hayes P, Matsuyama S. Cytoprotective membrane-permeable peptides designed from the Bax-binding domain of Ku70. Nat Cell Biol, 2003, 5(4): 352-357. [2].Rivas-Carrillo JD, Soto-Gutierrez A, Navarro-Alvarez N, et al. Cell-permeable pentapeptide V5 inhibits apoptosis and enhances insulin secretion, allowing experimental single-donor islet transplantation in mice. Diabetes, 2007, 56(5): 1259-1267. |
Cas No. | 579492-81-2 | SDF | |
别名 | BIP-V5; BAX Inhibiting Peptide V5 | ||
化学名 | (S)-6-amino-2-((Z)-((S)-2-((Z)-((S)-2-((Z)-(((S)-1-((S)-2-amino-3-methylbutanoyl)pyrrolidin-2-yl)(hydroxy)methylene)amino)-1-hydroxy-4-(methylthio)butylidene)amino)-1-hydroxy-4-methylpentylidene)amino)hexanoic acid | ||
Canonical SMILES | CC(C[C@@](/N=C(O)/[C@](/N=C(O)/[C@]1([H])CCCN1C([C@](N)([H])C(C)C)=O)([H])CCSC)([H])/C(O)=N/[C@@](C(O)=O)([H])CCCCN)C | ||
分子式 | C27H50N6O6S | 分子量 | 586.79 |
溶解度 | ≥ 29.35mg/mL in DMSO, ≥ 91.4 mg/mL in Water | 储存条件 | Desiccate at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.7042 mL | 8.5209 mL | 17.0419 mL |
5 mM | 0.3408 mL | 1.7042 mL | 3.4084 mL |
10 mM | 0.1704 mL | 0.8521 mL | 1.7042 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet