Pepstatin A
(Synonyms: 抑肽素; Pepstatin A) 目录号 : GC11974Pepstatin A (Pepstatin A A) 是一种由放线菌产生的特异性天冬氨酸蛋白酶抑制剂，对血红蛋白-胃蛋白酶、血红蛋白-蛋白酶、酪蛋白-胃蛋白酶、酪蛋白的 IC50 分别为 4.5 nM、6.2 nM、150 nM、290 nM、520 nM 和 260 nM -proctase，酪蛋白酸蛋白酶和血红蛋白酸蛋白酶，分别。
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
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Purity: >98.00%
- COA (Certificate Of Analysis)
- Datasheet
| Kinase experiment [1]: | |
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Binding assays |
The inhibition of HIV protease, pepsin and cathepsin D activities was assayed using the solid-phase immunoassay at pH 5.6. After induction and harvesting, cells (50 g) were resuspended in 100 ml of 10 mM Tris-HCl buffer, pH 7.5, 1 mM EDTA, 1 mM DTT, 1 mM PMSF and 0.05% Triton X-100, sonicated and centrifuged at 10000g for 20 min, HIV-I protease activity in E. coli extracts was assayed by cleavage of a synthetic heptapeptide substrate and HPLC analysis of proctucts. |
| Cell experiment [2, 3]: | |
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Cell lines |
H9 cells, Bone marrow cells |
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Preparation method |
The solubility of this compound in DMSO is >34.3mg/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. |
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Reacting condition |
0.1 mM for 2, 4, or 11 days, 37 ℃ |
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Applications |
Pepstatin A inhibited the proteolytic processing of the HIV gag precursor in H9 cells. Pepstatin A inhibited the production of infectious HIV in H9 cell cultures. Pepstatin A (15–120 μM) dose-dependently suppressed the formation of TRAP-positive multinuclear cells. Pepstatin A dose-dependently suppressed the RANKL-induced osteoclastogenesis from stromal cell–deprived bone marrow cells in the co-culture system and bone marrow culture. Pepstatin A (15 μM) substantially inhibited the aspartic proteinase activity in bone marrow cells, while complete inhibition was seen at 90 μM. |
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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. |
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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. > |
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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.>
| Cas No. | 26305-03-3 | SDF | |
| 别名 | 抑肽素; Pepstatin A | ||
| 化学名 | 3-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 | ||
| Canonical SMILES | CC(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 | ||
| 分子式 | C34H63N5O9 | 分子量 | 685.9 |
| 溶解度 | ≥ 34.3mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. | ||
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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| 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 % ddH2O | ||||||||||
| 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 ddH2O，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。