Calpeptin is a potent, cell-permeable calpain inhibitor with ID50 of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets), respectively.
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产品名称 | Cysteine Protease ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Z-FA-FMK | ✔ | 99%+ | |||||||||||||||||
Leupeptin hemisulfate | ✔ | 97% | |||||||||||||||||
PMSF | ✔ | 95% | |||||||||||||||||
PD 151746 |
+
μ-Calpain, IC50: 260 nM m-calpain, IC50: 5.33 μM |
98% | |||||||||||||||||
Odanacatib |
++++
Cathepsin K (rabbit), IC50: 1 nM Cathepsin K (human), IC50: 0.2 nM |
99%+ | |||||||||||||||||
E-64 |
+++
Cysteine protease, IC50: 9 nM |
99%+ | |||||||||||||||||
E 64c | ✔ | 95% | |||||||||||||||||
E-64d | ✔ | 99%+ | |||||||||||||||||
MG-101 | ✔ | 98%+ | |||||||||||||||||
Calpeptin |
++
Calpain II (porcine kidney), ID50: 40 nM Calpain I (porcine erythrocytes), ID50: 52 nM |
98%+ | |||||||||||||||||
Cathepsin inhibitor 1 |
+++
Cathepsin L2, pIC50: 5.5 Cathepsin L, pIC50: 7.9 |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
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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 |
Dose | Mice: 10 mg/kg[3] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 117591-20-5 |
分子式 | C20H30N2O4 |
分子量 | 362.463 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Store in freezer, under -20°C |
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 |