Date published: 2025-10-13

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Calpain 5 Activators

Calpain 5 Activators encompass a range of compounds that indirectly or directly enhance the functional activity of Calpain 5, a calcium-dependent cysteine protease involved in various cellular processes. The activation of Calpain 5 is intricately linked to intracellular calcium levels. Compounds like Calcium chloride anhydrous, Ionomycin, and A23187 are direct activators, increasing intracellular calcium concentrations, thereby facilitating the conformational changes necessary for Calpain 5 activation. Thapsigargin and (±)-Bay K 8644 also play significant roles; Thapsigargin by inducing calcium release from the endoplasmic reticulum and (±)-Bay K 8644 through its agonistic action on calcium channels, both leading to enhanced Calpain 5 activity. Additionally, (R)-(-)-Phenylephrine hydrochloride, through its agonistic effect on α1-adrenergic receptors, indirectly increases intracellular calcium, contributing to Calpain 5 activation. Further influencing Calpain 5 activity are compounds that modulate calcium dynamics indirectly. Chelerythrine chloride, by inhibiting Protein Kinase C, can affect calcium channel activity and thus influence Calpain 5 activation. Paradoxically, calcium channel blockers like Nifedipine, Nimodipine, and Verapamil can lead to a compensatory release of calcium from internal stores, potentially enhancing Calpain 5 activity. Ryanodine and Dantrolene, each affecting the ryanodine receptors and SERCA channels, modulate intracellular calcium levels, further contributing to the regulation of Calpain 5's protease activity. Collectively, these Calpain 5 Activators, through their diverse and complex mechanisms of modulating calcium homeostasis, underscore the critical role of calcium signaling in the regulation of Calpain 5, highlighting its importance in various cellular functions and signaling pathways.

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