Table 1.
CRAC channel modulators. This table summarizes the most common CRAC channel modulators together with their empirical formula, the function of interest and some additional information.
| Name | Empirical Formula | Function of Interest | Additional Information | References |
|---|---|---|---|---|
| 2-APB | (C6H5)2BOCH2CH2NH2 | Modulates: SOCE function in a concentration dependent manner | Activates: CRAC/STIM1 + Orai1 < 10 µM and Orai3 Blocks: CRAC/STIM1 + Orai1 > 50 µM Modulates: TRPV and TRPM channels |
[206] |
| BTP2 | C15H9F6N5OS | Blocks: CRAC Channel | Blocks: TPRC3 channel inhibitor and reduces NFAT nuclear translocation and cytokine production | [234] |
| SKF-96365 | C22H26N2O3 · HCl | Blocks: receptor-mediated Ca2+ entry | Blocks: voltage-gated Ca2+ entry; TRPC channel | [235] |
| GSK-5498A | C18H11F6N3O | Blocks: CRAC channel | - | [223] |
| GSK-5503A | C23H17F2N3O2 | Blocks: CRAC channel | - | [224] |
| GSK-7975A | C18H12F5N3O2 | Blocks: Orai1 | - | [222] |
| Synta66 | C20H17FN2O3 | Blocks: CRAC channel | No effect on L-type Ca2+ channel either TRPC1/5 | [236] |
| Pyr6 | C17H9F7N4O | Blocks: SOCE | Effect on carbachol-induced, TRPC3-mediated calcium entry inhibits the typical Orai downstream signaling cascades in RBL mast cells (NFAT activation and degranulation) |
[219] |
| Pyr10 | C18H13F6N3O2S | Blocks: CRAC channel | TRP cation 3 (TRPC3) inhibitor | [219] |
| RO2959 | C21H19F2N5OS.xHCl | Blocks: SOCE | Potent inhibitor of human IL-2 production, potently blocks T-cell receptor-triggered gene expression and T-cell functional pathways | [231] |