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Pepstatin A

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Chemical Structure| 26305-03-3 同义名 : 胃酶抑素A ;Pepstatin;NSC 272671;Pepstatinum;Pepsin Inhibitor S 735A
CAS号 : 26305-03-3
货号 : A135194
分子式 : C34H63N5O9
纯度 : 99%+
分子量 : 685.892
MDL号 : MFCD00060740
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(43.74 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Aspartic proteinases are a class of enzymes commonly expressed in osteoclasts that contribute to bone resorption in endosome/lysosome system. Pepstatin A is a chemotactic pentapeptide that inhibits different kinds of aspartic proteinases, such as pepsin, cathepsins D and E. In a co-culture system, Pepstatin A at 15 - 120 μM suppressed the formation of TRAP-positive multinuclear cells in a dose-dependent manner. Pepstatin A at the same concentration range also exhibited a similar inhibitory effect on RANKL/M-CSF-induced osteoclastogenesis in bone marrow culture. In bone marrow cells separated from stromal cells on a Sephadex G-10 column, pepstatin A at 15 - 120 μM dose-dependently suppressed RANKL-induced osteoclastogenesis. In osteoclasts generated from bone marrow cells and stimulated with RANKL and M-CSF, pepstatin A at 120 μM strongly inhibited the early stage of osteoclast formation. Pepstatin A at 15 μM sufficiently inhibited the aspartic proteinase activity in bone marrow cells and the complete inhibition was seen at the concentration of 90 μM. Additionally, pretreatment of pepstatin A for 3 hours inhibited RANKL-induced ERK activation and NFATc1 expression in osteoclasts[3]. Pepstatin A stimulated human neutrophil degranulation and superoxide production with EC50 values of 0.75 μM and 1.5 μM respectively[4].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human MCF7 cells Function assay Inhibition of cathepsin D in human MCF7 cells by fluorescence assay, IC50=0.005 μM 19715320
human MCF7 cells Function assay 1 h Inhibition of cathepsin D in human MCF7 cells treated for 1 hr measured after washout and trypsin treatment by fluorescence assay, IC50=5 μM 19715320
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.46mL

0.29mL

0.15mL

7.29mL

1.46mL

0.73mL

14.58mL

2.92mL

1.46mL
参考文献

[1]Yoshida H, Okamoto K, et al. Pepstatin A, an aspartic proteinase inhibitor, suppresses RANKL-induced osteoclast differentiation. J Biochem. 2006 Mar;139(3):583-90.

[2]Seelmeier S, Schmidt H, et al. Human immunodeficiency virus has an aspartic-type protease that can be inhibited by pepstatin A. Proc Natl Acad Sci U S A. 1988 Sep;85(18):6612-6.

[3]Yoshida H, Okamoto K, Iwamoto T, Sakai E, Kanaoka K, Hu JP, Shibata M, Hotokezaka H, Nishishita K, Mizuno A, Kato Y. Pepstatin A, an aspartic proteinase inhibitor, suppresses RANKL-induced osteoclast differentiation. J Biochem. 2006 Mar;139(3):583-90. doi: 10.1093/jb/mvj066. PMID: 16567424.

[4]Smith RJ, Bowman BJ, Iden SS, Kolaja GJ, Wiser SK. Biochemical, metabolic and morphological characteristics of human neutrophil activation with pepstatin A. Immunology. 1983 Jun;49(2):367-77. PMID: 6303951; PMCID: PMC1454214.