Small-molecule Inhibitors of Store-operated Calcium Entry
Inhibitor type | Species | Description | Reference |
---|---|---|---|
Direct channel inhibitors | Lanthanides | Potent and relatively specific inhibitors (effective at ~ 0.1 –1.0 μM) | (4, 59) |
2-APB | Relatively non-specific (effective at ~30 μM) | (3) | |
Analogs of APB (“improved”) | Improved potency/specificity (effective at ~ 0.6 6.6 μM) | (79) | |
Mechanism-based inhibitors | Nocodazole | Microtubule disrupter ~ 10 μM; however, inhibition is incomplete | (60) |
ML-9 | Inhibits STIM translocation, not through MLCK inhibition; (~10 μM) | (64) | |
2-APB | Weakly inhibits STIM translocation (~ 10 100 μM) | (48) | |
Mechanism not known | BTPs | Also activate TRPM4 | (83, 103) |
Synta66 | (102) | ||
Other recently described small molecules | [See (92)] | ||
Relatively non-specific inhibitors | [See (3)] |