Pepstatin A
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
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Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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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. Shuzhen Liu, Preston Perez, et al. "MLKL polymerization-induced lysosomal membrane permeabilization promotes necroptosis." Cell Death Differ. 2023 Nov 23. PMID: 37996483
- 2. 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
- 3. 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
- 4. Adams MK, Belyaeva OV, et al. "Generation and isolation of recombinant retinoid oxidoreductase complex." Methods Enzymol. 2020;637:77-93. PMID: 32359661
- 5. HeLia, GuanghuiDanga, et al. "Characterization of a novel Mycobacterium tuberculosis serine protease (Rv3194c) activity and pathogenicity." Tuberculosis. Available online 4 November 2019, 101880.
- 6. 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]: | |
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]: | |
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°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。 |
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. > |
质量控制和MSDS
- 批次:
化学结构
![Pepstatin A](https://www.apexbt.com/media/diy/images/struct/A2571.png)
相关生物数据
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