Pepstatin A
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Pepstatin A（胃蛋白酶抑制素A）是公认的天冬氨酸蛋白酶的抑制剂，对人肾素、HIV蛋白酶、胃蛋白酶和组织蛋白酶D的IC50值分别为15 μM，2 μM，<5 μM和 <40 μM [1,2]。
胃蛋白酶抑制素A是一种五肽。它最初是从微生物分离得到的。作为一种最有效的肾素抑制剂，在弱酸性条件下，pepstatin A抑制猪肾素和人类肾素， IC50值分别为0.32和15 μM。其缺点是，胃蛋白酶抑制剂具有一定的疏水性。使用亲水性残基耦合pepstatin A的C末端可以增加其溶解度。除了抑制肾素之外，胃蛋白酶抑制剂A对HIV蛋白酶也具有一定的抑制作用，最终抑制病毒的复制。在培养的H9细胞，给予pepstatin A可以阻断病毒前体的蛋白水解，最终抑制感染性病毒HIV的产生。研究表明，胃酶抑素A通过抑制组织蛋白酶D和E能抑制破骨细胞分化 [1,3,4]。
参考文献：
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.
- 1. Banghao Yuan, Caroline Hatchett-Walker, et al. "Coronaviruses exploit a host cysteine-aspartic protease for replication." J Biol Chem. 2022 Oct 13;102590. PMID: 36244453
- 2. Yan Chen, Jiafu Zhu, et al. "Protocol for affordable and efficient profiling of nascent RNAs in bread wheat using GRO-seq." STAR Protoc. 2022 Sep 16;3(3):101657. PMID: 36097381
- 3. HeLia, GuanghuiDanga, et al. "Characterization of a novel Mycobacterium tuberculosis serine protease (Rv3194c) activity and pathogenicity." Tuberculosis. Available online 4 November 2019, 101880.
- 4. 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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 685.9 |
| Cas No. | 26305-03-3 |
| Formula | C34H63N5O9 |
| Synonyms | Pepstatin A,NSC272671,Isoval-Val-Val-Sta-Ala-Sta |
| Solubility | ≥34.3 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | 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 |
| SDF | Download SDF |
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 激酶实验[1]: | |
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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，10000 g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]: | |
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细胞系 |
H9细胞，骨髓细胞 |
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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°C下孵育10分钟，随后在超声波浴中摇匀。-20°C以下可储存数月。 |
|
反应时间 |
0.1 mM，2、4或11天，37 °C |
|
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。 |
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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。 |
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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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质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
