55123-66-5
Chemical Structure
Leupeptin
- CAS No.: 55123-66-5
- Formula:C20H38N6O4
- Molecular Weight:426.55
IUPAC Name: (S)-2-acetamido-N-((S)-1-(((S)-5-guanidino-1-oxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)-4-methylpentanamide
InChIKey: GDBQQVLCIARPGH-ULQDDVLXSA-N
SMILES: O=C[C@@H](NC([C@@H](NC([C@@H](NC(C)=O)CC(C)C)=O)CC(C)C)=O)CCCNC(N)=N
Biological Activity: Leupeptin is a broad-spectrum protease inhibitor. By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin can be used in research on chronic inflammatory diseases and skin tumorigenesis[1][2][3][4].
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Leupeptin | Leupeptin is a broad-spectrum protease inhibitor. By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin can be used in research on chronic inflammatory diseases and skin tumorigenesis. | |||||||||||||||||||||
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References
- [1]. Sharma A, et al. Leupeptin maintains redox homeostasis via targeting ROS-autophagy-inflammatory axis in LPS-stimulated macrophages and cytokines dichotomy in Con-A challenged lymphocyte. Peptides. 2023 Oct;168:171066. [Content Brief]
- [2]. Hozumi M, et al. Inhibition of tumorigenesis in mouse skin by leupeptin, a protease inhibitor from Actinomycetes. Cancer Res. 1972 Aug;32(8):1725-8. [Content Brief]
- [3]. Haspel J, et al. Characterization of macroautophagic flux in vivo using a leupeptin-based assay. Autophagy. 2011 Jun;7(6):629-42. [Content Brief]
- [4]. Billinger E, et al. Inhibition properties of free and conjugated leupeptin analogues. FEBS open bio. 2020 Dec;10(12):2605-2615. [Content Brief]