| Name | Zegocractin |
| Description | Zegocractin (CM-4620) is an inhibitor of calcium-release activated calcium (CRAC) channels. |
| In vitro | CM-4620 (compound 1) is more potent on Orai1 than Orai2-type CRAC channels. In human PBMCs, CM-4620 potently inhibits release of multiple cytokines which play important roles in T cells (IC50s, IFN γ: 138 nM, IL-6: 135 nM, IL-4: 879 nM, IL-1β: 240 nM, IL-10: 303 nM, IL-2: 59 nM, TNFα: 225 nM, IL-17 120 nM) [1]. |
| In vivo | Mouse PACs are treated with CRAC inhibitors GSK-7975A or CM-4620 and monitored for their rate of Calcium uptake. Both CRAC inhibitors reduce the rate of store-operated Calcium entry into the ER to 50% of control levels upon treatment with 700 nM of inhibitor. CM-4620 blocks 100% of the reuptake at 10 mM. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+90% Corn Oil : 3.3 mg/mL (7.82 mM), Sonication is recommended. H2O : Insoluble DMSO : 140 mg/mL (331.94 mM), Sonication is recommended.
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| Keywords | Zegocractin | Orai2/STIM1 | Orai1/STIM1 | Inhibitor | inhibit | CRAC Channel | CM 4620 | CalciumChannel | Calcium release-activated channels | Calcium Channel | Ca2+ release-activated Ca2+ channels |
| Inhibitors Related | Quadrol | Tricaine methanesulfonate | Nisoldipine | 2,4,6-Tri-tert-butylphenol | Chlorocresol | L-Ascorbic acid | L-Phenylalanine | L-Ascorbic acid sodium salt | 1-Octanol | 2-Nitrobenzoic acid | Magnesium Chloride Hexahydrate | Magnesium sulfate |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Neuroprotective Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Drug Library |