切换导航

Pepstatin A

现货
Catalog No.
A2571
天冬氨酸蛋白酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 500.00
现货
10mg
¥ 450.00
现货
50mg
¥ 1,600.00
现货
100mg
¥ 2,800.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

Pepstatin A is a well-known inhibitor of aspartic proteinases with IC50 values of 15 μM, 2 μM, < 5 nM and < 40 nM for human renin, HIV protease, pepsin and cathepsin D, respectively [1, 2].

Pepstatin A is a pentapeptide. It was originally isolated from the microbe. As a most potent renin inhibitor, pepstatinA inhibited porcine renin and human renin at weak acid pH value with IC50 values of 0.32 and 15 μM, respectively. The disadvantage is that, pepstatin Ais hydrophobic. To couple the charged hydrophilic residues to the C-terminal of pepstatinA can increase its solubility. Besides the renin, pepstatin A was also reported to have inhibitory effects on HIV protease and subsequently suppressed the virus replication. In cultured H9 cells, pepstatinA treatment blocked the proteolytic processing of the virus gag precursor and inhibited the production of infectious HIV. Moreover, pepstatin A was found to inhibit osteoclast differentiation due to its inhibitory efficacy of cathepsin D and E [1, 3 and 4].

References:
1. Eid M, Evin G, Castro B, et al.New renin inhibitors homologous with pepstatin.Biochem. J, 1981, 197: 465-471.
2. Sarubbi E, Seneci P F, Angelastro M R, et al. Peptide aldehydes as inhibitors of HIV protease. FEBS letters, 1993, 319(3): 253-256.
3. von der Helm K, Gürtler L, Eberle J, et al. Inhibition of HIV replication in cell culture by the specific aspartic protease inhibitor pepstatin A. FEBS letters, 1989, 247(2): 349-352.
4. Yoshida H, Okamoto K, Iwamoto T, et al. Pepstatin A, an aspartic proteinase inhibitor, suppresses RANKL-induced osteoclast differentiation. Journal of biochemistry, 2006, 139(3): 583-590.>

文献引用

1. Ying Long, Xuri Zhang, et al. "Initial events in the breakthrough of the epithelial barrier of the small intestine by Angiostrongylus cantonensis." Arch Biol Sci. 2016;68(2):375-383

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt685.9
Cas No.26305-03-3
FormulaC34H63N5O9
SynonymsPepstatin A,NSC272671,Isoval-Val-Val-Sta-Ala-Sta
Solubility≥34.3mg/mL in DMSO
Chemical Name3-hydroxy-4-[2-[[3-hydroxy-6-methyl-4-[[3-methyl-2-[[3-methyl-2-(3-methylbutanoylamino)butanoyl]amino]butanoyl]amino]heptanoyl]amino]propanoylamino]-6-methylheptanoic acid
SDFDownload SDF
Canonical SMILESCC(C)CC(C(CC(=O)O)O)NC(=O)C(C)NC(=O)CC(C(CC(C)C)NC(=O)C(C(C)C)NC(=O)C(C(C)C)NC(=O)CC(C)C)O
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

激酶实验[1]:

激酶实验

使用pH 5.6的固相免疫测定法测定HIV蛋白酶,胃蛋白酶和组织蛋白酶D活性的抑制。诱导和收获细胞后,将细胞重悬于100 ml 10 mM Tris-HCl、pH 7.5、1 mM EDTA、1 mM DTT、1 mM PMSF和0.05% Triton X-100缓冲液中,超声处理,10000g离心20 min,大肠杆菌提取物中的HIV-1蛋白酶活性通过合成七肽底物的切割和对产物进行HPLC分析来测定。

细胞实验 [2, 3]:

细胞系

H9细胞,骨髓细胞

溶解方法

该化合物在DMSO中的溶解度大于34.3 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。

反应时间

0.1 mM,2、4或11天,37 ℃

应用

Pepstatin A抑制H9细胞中HIV gag前体的蛋白水解加工。Pepstatin A抑制H9细胞培养物中感染性HIV的产生。Pepstatin A(15-120 μM)以剂量依赖性方式抑制TRAP阳性多核细胞的形成。在共培养系统和骨髓培养物中,Pepstatin A以剂量依赖性方式抑制RANKL诱导的从基质细胞剥夺的破骨细胞发生。Pepstatin A(15 μM)抑制骨髓细胞中的天冬氨酸蛋白酶活性,90 μM的Pepstatin A几乎完全抑制天冬氨酸蛋白酶活性。

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]. Sarubbi E, Seneci P F, Angelastro M R, et al. Peptide aldehydes as inhibitors of HIV protease. FEBS letters, 1993, 319(3): 253-256.

[2]. von der Helm K, Gürtler L, Eberle J, et al. Inhibition of HIV replication in cell culture by the specific aspartic protease inhibitor pepstatin A. FEBS letters, 1989, 247(2): 349-352.

[3] Yoshida H, Okamoto K, Iwamoto T, et al. Pepstatin A, an aspartic proteinase inhibitor, suppresses RANKL-induced osteoclast differentiation. Journal of biochemistry, 2006, 139(3): 583-590. >

质量控制

化学结构

Pepstatin A

相关生物数据

CORM-3