Pharmacology of Store-operated Calcium Channels

Table 1

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)]