Calpain
calcium-activated neutral cysteine protease
Calpain is a widely expressed cytosolic cysteine protease; its substrate recognition sequences differ from those of caspases, and it exists as two isoforms (Calpain I and Calpain II) with distinct requirements for calcium ions. It is activated by elevated intracellular calcium concentrations; consequently, it becomes activated and participates in the process of cell death in various cell types exposed to apoptotic signals. However, calpain is not a prerequisite for all apoptotic events; for instance, while it is essential for specific instances of apoptosis induction in thymocytes and hepatocytes, it is not required for Fas-induced apoptosis in Jurkat cells. Furthermore, calpain-mediated proteolytic cleavage is implicated in both necrotic and apoptotic processes associated with neurodegenerative diseases, such as cerebral ischemia and Alzheimer's disease[1].
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Calpain Related Products (4)
Related Products (4)
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CAST-calpain-2 stabilizer-1
0 ImagesCAST-calpain-2 stabilizer-1 is a blood-brain barrier permeable stabilizer of CAST-calpain-2 interaction. CAST-calpain-2 stabilizer-1 shows no activity against GSK3. CAST-calpain-2 stabilizer-1 can be used in the research of Huntington's disease and tauopathies.
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SNJ-1945
0 ImagesSNJ-1945 is an orally active, blood-brain barrier-penetrant Calpain inhibitor. SNJ-1945 inhibits Cathepsin L, Cathepsin B, and Ca2+ -independent proteases. SNJ-1945 suppresses ROS production and downregulates Cyclooxygenase-2 and Caspase-1. SNJ-1945 alleviates left ventricular systolic dysfunction, reduces cerebral ischemia-induced injury, and decreases the score of experimental autoimmune encephalomyelitis in mouse models. SNJ-1945 can be used in research related to post-cardiac arrest reperfusion injury, Parkinson's disease, multiple sclerosis, and proliferative retinopathy.
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N-Acetyl-L-leucyl-L-leucyl-L-methional
0 ImagesCat. No.: HY-103321CAS No.: 145757-50-2N-Acetyl-L-leucyl-L-leucyl-L-methional is a Calpain II inhibitor with an IC50 of 0.24 μM against porcine Calpain II. N-Acetyl-L-leucyl-L-leucyl-L-methional forms a stable tetrahedral adduct with the thiol group at the active site of Calpain II, thereby inhibiting proteolytic activity. N-Acetyl-L-leucyl-L-leucyl-L-methionally inhibits cathepsins in a non-selective manner. N-Acetyl-L-leucyl-L-leucyl-L-methional reduces SARS-CoV-2 infection levels in human coronary artery endothelial cells in vitro. N-Acetyl-L-leucyl-L-leucyl-L-methional can be used in research related to cataracts and coronavirus infections.
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Ibulocydine
0 ImagesCat. No.: HY-116054CAS No.: 1314096-68-8Ibulocydine is an isobutyrate prodrug of the Cdk inhibitor BMK-Y101 (HY-188159), with oral activity, and exhibits IC50 values of approximately 50 nM against CDK1/CDK2, 530 nM against CDK7/cyclin H/Mat1, and 85 nM against CDK9/cyclin T. Ibulocydine reduces the phosphorylation levels of Rb, nucleolin, and RNA polymerase II CTD Ser-5 and Ser-2, downregulates the expression of Mcl-1, survivin, and XIAP, decreases MMP-9 expression, and lowers the Bcl-2/Bax ratio, activates calpain-mediated Bax cleavage, cytochrome c release, and caspase activation. Ibulocydine induces apoptosis, inhibits the growth of cancer cells and xenografts, enhances the sensitivity of cancer cells to TRAIL and radiotherapy, and blocks cancer cell metastasis. Ibulocydine can be used in research related to various cancers, including hepatocellular carcinoma, triple-negative breast cancer, lung cancer, and colon cancer.
