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Calpeptin

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Chemical Structure| 117591-20-5 同义名 : -
CAS号 : 117591-20-5
货号 : A590110
分子式 : C20H30N2O4
纯度 : 98%+
分子量 : 362.463
MDL号 : MFCD00155623
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(289.68 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
靶点

  • Cysteine Protease

    Calpain I (porcine erythrocytes), ID50:52 nM

    Calpain II (porcine kidney), ID50:40 nM
描述 Calpain is a Ca2+-mediated cytosolic cyctein protease existed in various cells. Calpeptin is a potent calpain inhibitor with ID50 values of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papain, and Calpain I (human platelets), respectively. In platelets stimulated by A23187, 66% of ABP and 69% of P235 remained undegraded in the presence of 10μg/mL calpeptin, in comparison to 26% of ABP and 40% of P235 remained without calpeptin. The activity of intrinsic calpain in platelets was completely abolished by the treatment of 100μg/mL calpeptin[4]. Calpeptin at the concentration of 34nM reduced calpain activity by 44% in the homogenate of proliferating PC12 cells. When PCI2 cells were incubated with NGF and 36μM calpeptin for 17h, the probabilities for a PCI2 cell to extend a given maximal neurite length were increased as compared to non-calpeptin-treated cells[5]. In a murine model of middle cerebral artery occlusion, the intra-cerebroventricle injection of calpeptin (50μg dissolved in 5μL DMSO) before the occlusion resulted in a significant reduction of neuronal apoptosis in hippocampal CA1 sector, as compared to DMSO-treated animals, via the inhibition of caspase-3 expression[6].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
COS7 cells 50 μM Function assay 24 h Induction of autophagy in african green monkey COS7 cells assessed as increase in autophagosome at 50 uM after 24 hrs by electron microscopy 18391949
HeLa cells 50 μM Function assay Induction of autophagy in human HeLa cells expressing EGFP-LC3 assessed as increase in LC3-2 level at 50 uM in presence of 400 nM bafilomycin A1 18391949
PC12 cells 10 μM Function assay 96 h Induction of autophagy in undifferentiated rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 10 uM after 96 hrs by calpain activation assay 18391949
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.76mL

0.55mL

0.28mL

13.79mL

2.76mL

1.38mL

27.59mL

5.52mL

2.76mL
参考文献

[1]Pinter M, Aszodi A, et al. Calpeptin, a calpain inhibitor, promotes neurite elongation in differentiating PC12 cells. Neurosci Lett. 1994 Mar 28;170(1):91-3.

[2]Tsujinaka T, Kajiwara Y, et al. Synthesis of a new cell penetrating calpain inhibitor (calpeptin). Biochem Biophys Res Commun. 1988 Jun 30;153(3):1201-8.

[3]Jorfi S, Ansa-Addo EA, et al. Inhibition of microvesiculation sensitizes prostate cancer cells to chemotherapy and reduces docetaxel dose required to limit tumor growth in vivo. Sci Rep. 2015 Aug 25;5:13006.

[4]Tsujinaka T, Kajiwara Y, Kambayashi J, Sakon M, Higuchi N, Tanaka T, Mori T. Synthesis of a new cell penetrating calpain inhibitor (calpeptin). Biochem Biophys Res Commun. 1988 Jun 30;153(3):1201-8. doi: 10.1016/s0006-291x(88)81355-x. PMID: 2839170.

[5]Pintér M, Aszódi A, Friedrich P, Ginzburg I. Calpeptin, a calpain inhibitor, promotes neurite elongation in differentiating PC12 cells. Neurosci Lett. 1994 Mar 28;170(1):91-3. doi: 10.1016/0304-3940(94)90246-1. PMID: 8041520.

[6]Peng S, Kuang Z, Zhang Y, Xu H, Cheng Q. The protective effects and potential mechanism of Calpain inhibitor Calpeptin against focal cerebral ischemia-reperfusion injury in rats. Mol Biol Rep. 2011 Feb;38(2):905-12. doi: 10.1007/s11033-010-0183-2. Epub 2010 May 16. PMID: 20473717.