Calpain Inhibitor I, ALLN
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Calpain Inhibitor I是钙蛋白酶I、钙蛋白酶II、组织蛋白酶B和组织蛋白酶L的抑制剂，Ki值分别为190 nM、220 nM、150 nM和500 pM。
在DLD1-TRAIL/R细胞中，calpain inhibitor I与Ad/gTRAIL联合使用可诱导细胞急剧死亡，而calpain inhibitor I单独使用只有最小的杀伤作用。Calpain inhibitor I与TRAIL蛋白联合使用导致caspase-8和caspase-3切割成其活性形式[1]。
在雄性Sprangue-Dawley大鼠中，calpain inhibitor I减少P-selectin/ICAM-1表达、中性粒细胞浸润、脂质过氧化、硝基酪氨酸、PAR形成以及IκB-α降解[2]。
参考文献：
[1] Zhu H1,?Zhang L,?Huang X,?Davis JJ,?Jacob DA,?Teraishi F,?Chiao P,?Fang B. Overcoming acquired resistance to TRAIL by chemotherapeutic agents and calpain inhibitor I through distinct mechanisms. Mol Ther.?2004 May;9(5):666-73.
[2] Marzocco S1,?Di Paola R,?Autore G,?Mazzon E,?Pinto A,?Caputi AP,?Thiemermann C,?Cuzzocrea S. Calpain inhibitor I reduces intestinal ischemia-reperfusion injury in the rat. Shock.?2004 Jan;21(1):38-44.
- 1. Vimala Bondada, Jozsef Gal, et al. "The C2 domain of calpain 5 contributes to enzyme activation and membrane localization." Biochim Biophys Acta Mol Cell Res. 2021 Jun;1868(7):119019. PMID: 33811937
- 2. Andrew R Ednie, Eric S Bennett. "Intracellular O-linked glycosylation directly regulates cardiomyocyte L-type Ca 2+ channel activity and excitation–contraction coupling." Basic Res Cardiol. 2020 Sep 10;115(6):59. PMID: 32910282
- 3. Ednie AR, Parrish AR, et al. "Reduced hybrid/complex N-glycosylation disrupts cardiac electrical signaling and calcium handling in a model of dilated cardiomyopathy." J Mol Cell Cardiol. 2019 Jul;132:13-23. PMID: 31071333
- 4. YU HUANG. "STUDY OF REGULATED CELL DEATH IN TWO SYSTEMS: PD-1 IN NATURAL KILLER CELLS AND RIP3 IN NEURONS." The University of Texas. 2018.
- 5. KoraMagazi A, Wang D, et al. "Rhein triggers apoptosis via induction of endoplasmic reticulum stress, caspase-4 and intracellular calcium inprimary human hepatic HL-7702 cells." Biochem Biophys Res Commun. 2016 Apr 22;473(1):230-236. PMID: 27003256
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 383.54 |
| Cas No. | 110044-82-1 |
| Formula | C20H37N3O4 |
| Synonyms | Ac-LLnL-CHO, MG-101, MG101,N-Acetyl-L-leucyl-L-leucyl-L-norleucinal, N-Acetyl-Leu-Leu-Nle-al,Calpain Inhibitor I |
| Solubility | insoluble in H2O; ≥14.03 mg/mL in EtOH; ≥19.1 mg/mL in DMSO |
| Chemical Name | 2-acetamido-4-methyl-N-[4-methyl-1-oxo-1-(1-oxohexan-2-ylamino)pentan-2-yl]pentanamide |
| SDF | Download SDF |
| Canonical SMILES | CCCCC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
DLD1-TRAIL/R细胞 |
|
制备方法 |
在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液，一般步骤如下：请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
|
反应条件 |
0、10、20和50 μM；96小时 |
|
实验结果 |
在DLD1-TRAIL/R细胞中，Calpain Inhibitor I和Ad/gTRAIL联合用药显著诱导细胞死亡。当单独使用Calpain Inhibitor I和Ad/gTRAIL时，两者的作用最小。 |
| 动物实验 [2]: | |
|
动物模型 |
内脏动脉阻断性(SAO)休克大鼠 |
|
给药剂量 |
15 mg/kg；腹腔注射 |
|
实验结果 |
在再灌注前，先腹腔注射15 mg/kg Calpain Inhibitor I可以显著减少IκB-α降解、再灌注回肠中的P-选择素/ICAM-1强度，中性粒细胞浸润以及丙二醛水平。同时，Calpain Inhibitor I预处理显着改善平均动脉血压和再灌注组织的组织学状态。 |
|
其他注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
|
References: [1]. Zhu H1, Zhang L, Huang X, Davis JJ, Jacob DA, Teraishi F, Chiao P, Fang B. Overcoming acquired resistance to TRAIL by chemotherapeutic agents and calpain inhibitor I through distinct mechanisms. Mol Ther.?2004 May;9(5):666-73. [2]. Marzocco S1, Di Paola R, Autore G, Mazzon E, Pinto A, Caputi AP, Thiemermann C, Cuzzocrea S. Calpain inhibitor I reduces intestinal ischemia-reperfusion injury in the rat. Shock. 2004 Jan;21(1):38-44. | |
| 描述 | Calpain Inhibitor I,ALLN是calpain I、calpain II、cathepsin B和cathepsin L的抑制剂，Ki值分别为190 nM、220 nM、150 nM和500 pM。 | |||||
| 靶点 | calpain I | calpain II | cathepsin B | cathepsin L | ||
| IC50 | 190 nM(Ki) | 220 nM(Ki) | 150 nM(Ki) | 500 nM(Ki) | ||
质量控制和MSDS
- 批次:
化学结构
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