A2602-5mg | Calpain Inhibitor I, ALLN [110044-82-1] Quimigen Portugal

Calpain Inhibitor I is an inhibitor of calpain I, calpain II, cathepsin B and cathepsin L with Ki values of 190 nM, 220 nM, 150 nM and 500 pM, respectively.

Calpain inhibitor I combined with Ad/gTRAIL induced cell death dramatically in DLD1-TRAIL/R cells, while calpain alone had only minimal killing effects. The combination of calpain inhibitor I and TRAIL protein resulted in cleavage of both caspase-8 and caspase-3 to active subunits [1].

Calpain inhibitor I treated male Sprangue-Dawley rats have seen reductions of P-selectin/ICAM-1 expression, neutrophil infiltration, lipid peroxidation, nitrotyrosine, PAR formation as well as IκB-α degradation [2].

Reference:
[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
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Cell experiment [1]:
Cell lines	DLD1-TRAIL/R cells
Preparation method	The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reaction Conditions	0, 10, 20 and 50 μM; 96 hrs
Applications	In DLD1-TRAIL/R cells, Calpain Inhibitor I combined with Ad/gTRAIL induced cell death dramatically while Calpain Inhibitor I or Ad/gTRAIL alone only had minimal killing effects.
Animal experiment [2]:
Animal models	Splanchnic artery occlusion (SAO)-shocked rats
Dosage form	15 mg/kg; i.p.
Applications	Calpain Inhibitor I, given intraperitoneally 30 mins before ischemia at a dose of 15 mg/kg, significantly reduced IκB-α degradation, the intensity of P-selectin/ICAM-1 in the reperfused ileum, neutrophil infiltration as well as malondialdehyde levels. Meanwhile, pretreatment of Calpain Inhibitor I markedly improved mean arterial blood pressure and the histological status of the reperfused tissue.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
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.

Description	Calpain Inhibitor I,ALLN is an inhibitor of calpain I, calpain II, cathepsin B and cathepsin L with Ki values of 190 nM, 220 nM, 150 nM and 500 pM, respectively
Targets	calpain I	calpain II	cathepsin B	cathepsin L
IC50	190 nM(Ki)	220 nM(Ki)	150 nM(Ki)	500 nM(Ki)

Purity = 98.00%

Calpain Inhibitor I, ALLN [110044-82-1]

Referência A2602-5mg

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