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Calpain Inhibitor II, ALLM

Catalog No.
A2603
Calpain inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$80.00
In stock
5mg
$50.00
In stock
25mg
$200.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Calpain inhibitor II (CPI-2) is a cell-permeable inhibitor of calpain I, calpan II, cathepsin L and cathepsin B. 

Calpain inhibitor II 2 at 50 or 100 μM has shown to induce apoptosis in (acute lymphoblastic leukemia) ALL (ALL-1, RS4;11, and JURKAT) and (non-Hodgkin’s lymphoma) NHL (RAMOS and DAUDI) cell lines, as measured by MC540 single fluorescence. Additionally, studies have shown that neither BTK nor LYN were required for calpain inhibitor II induced apoptosis. Calpain inhibition with calpain inhibitor II has been demonstrated to induce apoptosis-promoting caspase system [1]. Unlike calpain inhibitor I, calpain inhibitor II cannot inhibit NFkB and sensitize DLD1-TRAIL/R cells to the TRAIL protein [2].

References:
[1] Zhu DM1, Uckun FM. Calpain inhibitor II induces caspase-dependent apoptosis in human acute lymphoblastic leukemia and non-Hodgkin's lymphoma cells as well as some solid tumor cells. Clin Cancer Res. 2000 Jun;6(6):2456-63.
[2] 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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt401.57
Cas No.136632-32-1
FormulaC19H35N3O4S
SynonymsN-Acetyl-Leu-Leu-Methional
Solubilityinsoluble in H2O; ≥14.85 mg/mL in DMSO; ≥20.27 mg/mL in EtOH
Chemical Name2-acetamido-4-methyl-N-[4-methyl-1-[(4-methylsulfanyl-1-oxobutan-2-yl)amino]-1-oxopentan-2-yl]pentanamide
SDFDownload SDF
Canonical SMILESCC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CCSC)C=O)NC(=O)C
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

Acute lymphoblastic leukemia (ALL) cell lines (ALL-1, RS4;11, and JURKAT) and non-Hodgkin’s lymphoma (NHL) cell lines (RAMOS and DAUDI)

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

50 or 100 μM; 24 hrs

Applications

At the dose of 50 or 100 μM, Calpain inhibitor II induced apoptosis in ALL (ALL-1, RS4;11, and JURKAT) and NHL (RAMOS and DAUDI) cell lines. Additionally, studies had shown that neither BTK nor LYN were required for Calpain inhibitor II induced apoptosis. Calpain inhibition with Calpain inhibitor II had been demonstrated to activate an apoptosis-promoting caspase system.

References:

[1]. Zhu DM1, Uckun FM. Calpain inhibitor II induces caspase-dependent apoptosis in human acute lymphoblastic leukemia and non-Hodgkin's lymphoma cells as well as some solid tumor cells. Clin Cancer Res. 2000 Jun;6(6):2456-63.

Biological Activity

Description Calpain Inhibitor II, ALLM is a cell-permeable inhibitor of calpain I, calpain II, cathepsin L and cathepsin B with Ki values of 120 nM, 230 nM, 0.6 nM and 100 nM, respectively.
Targets calpain I calpain II cathepsin L cathepsin B    
IC50 120 nM (Ki) 230 nM (Ki) 0.6 nM (Ki) 100 nM (Ki)    

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