Calpain Inhibitor II, ALLM
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.
- 1. 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
- 2. 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
- 3. Li W, Liu BD, et al. "Alteration of Androgen Receptor Protein Stability by Triptolide in LNCaP Cells." Medicina (Kaunas). 2018 May 30;54(3). pii: E39. PMID: 30344270
- 4. Chen Y, Yu Y, et al. "Bradykinin promotes migration and invasion of hepatocellular carcinoma cells through TRPM7 and MMP2." Exp Cell Res. 2016 Sep 29. PMID: 27693494
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 401.57 |
| Cas No. | 136632-32-1 |
| Formula | C19H35N3O4S |
| Synonyms | N-Acetyl-Leu-Leu-Methional |
| Solubility | insoluble in H2O; ≥14.85 mg/mL in DMSO; ≥20.27 mg/mL in EtOH |
| Chemical Name | 2-acetamido-4-methyl-N-[4-methyl-1-[(4-methylsulfanyl-1-oxobutan-2-yl)amino]-1-oxopentan-2-yl]pentanamide |
| SDF | Download SDF |
| Canonical SMILES | CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CCSC)C=O)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]: | |
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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) |
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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. |
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Reaction Conditions |
50 or 100 μM; 24 hrs |
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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. |
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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. |
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| 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) | ||
Quality Control & MSDS
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