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Bax inhibitor peptide V5

现货
Catalog No.
A4461
Bax抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,450.00
现货
5mg
¥ 900.00
现货
10mg
¥ 1,470.00
现货
100mg
¥ 8,400.00
Ship with 10-15 days

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Background

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.

Chemical Properties

Physical AppearanceA solid
StorageDesiccate at -20°C
M.Wt586.79
Cas No.579492-81-2
FormulaC27H50N6O6S
Solubility≥29.35mg/mL in DMSO, <2.1 mg/mL in EtOH, ≥91.4 mg/mL in H2O
Chemical Name(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
SDFDownload SDF
Canonical SMILESCC(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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1,2]:

细胞系

鼠胰岛细胞

溶解方法

该化合物在DMSO中的溶解度大于24.1 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

0-100 μM,24 h

应用

在STF-cMyc细胞中,Bax inhibitor peptide V5 (BIP V5)(0-50 μM)降低细胞死亡,但对SW620或NCI-H23细胞没有影响。BIP V5对G2/M期的细胞周期停滞没有显著影响。在小鼠胰岛中,BIP V5(100 μM)上调抗凋亡蛋白Bcl-2和XIAP超过3和11倍,下调凋亡诱导蛋白Bax、Bad和核因子-κB-p65的表达分别为10%、30%和近50%。

动物实验 [2]:

动物模型

链脲佐菌素诱导的糖尿病小鼠

给药剂量

100 μmol/l

应用

在链脲佐菌素诱导的糖尿病小鼠中,移植150个BIP V5处理的胰岛等效物与450个未处理的对照胰岛等效物在调解血糖中的作用相当。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

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.

质量控制

化学结构

Bax inhibitor peptide V5