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Calpain-2-IN-1

目录号 : GC67908

Calpain-2-IN-1 (Formula 1A) 是一种 calpain-2 亚型特异性的抑制剂,对 calpain-1 和 calpain-2 的 Ki 分别为 181 nM 和 7.8 nM。Calpain-2-IN-1 可用于神经退行性疾病和其他突触功能疾病的研究。

Calpain-2-IN-1 Chemical Structure

Cas No.:144231-85-6

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1mg
¥1,963.00
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5mg
¥4,320.00
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10mg
¥7,380.00
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产品描述

Calpain-2-IN-1 (Formula 1A) is a isoform-specific calpain-2 inhibitor with Kis of 181 nM and 7.8 nM for calpain-1, and calpain-2, respectively. Calpain-2-IN-1 can be used for the research of neurodegenerative diseases and other diseases of synaptic function[1].

[1]. Michel Baudry, et al. Isoform-specific calpain inhibitors, methods of identification, and uses thereof. WO2016077461A2.

Chemical Properties

Cas No. 144231-85-6 SDF Download SDF
分子式 C28H37N3O7 分子量 527.61
溶解度 DMSO : 100 mg/mL (189.53 mM; Need ultrasonic) 储存条件 Store at -20°C
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1 mM 1.8953 mL 9.4767 mL 18.9534 mL
5 mM 0.3791 mL 1.8953 mL 3.7907 mL
10 mM 0.1895 mL 0.9477 mL 1.8953 mL
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Research Update

Calpain-2 Facilitates Autophagic/Lysosomal Defects and Apoptosis in ARPE-19 Cells and Rats Induced by Exosomes from RPE Cells under NaIO3 Stimulation

Oxid Med Cell Longev 2023 Jan 17;2023:3310621.PMID:36703913DOI:PMC9873447

Although accumulated evidence supports the notion that calpain contributes to eye disease, the mechanisms by which calpain promotes RPE injury are not defined. The present study is aimed at investigating whether the effect of NaIO3-exos (exosomes derived from RPE cells under NaIO3 stimulation) on the dysfunction of the autophagy-lysosomal pathway (ALP) and apoptosis is based on its regulation of calpain activation in ARPE-19 cells and rats. The results showed that calpain-2 activation, ALP dysfunction, and apoptosis were induced by NaIO3-exos in ARPE-19 cells. NaIO3-exo significantly increased autophagic substrates by activating lysosomal dysfunction. ALP dysfunction and apoptosis in vitro could be eliminated by knocking down calpain-2 (si-C2) or the inhibitor Calpain-2-IN-1. Further studies indicated that NaIO3-exo enhanced calpain-2 expression, ALP dysfunction, apoptosis, and retinal damage in rats. In summary, these results demonstrate for the first time that calpain-2 is one of the key players in the NaIO3-exo-mediated ALP dysfunction, apoptosis, and retinal damage and identify calpain-2 as a promising target for therapies aimed at age-related macular degeneration (AMD).