Skip to main content
. 2021 Nov 27;11(12):1781. doi: 10.3390/biom11121781

Table 4.

SOCs inhibitors used as research tool.

Compound Mode of Action IC50 Side Effects References
Orai1 Inhibitor
YM-58483 (BTP2 or Pyr2) - 10–590 nM Inhibits TRPC3 and -C6 (IC50: 0.3 µM)
Activates TRPM4 channels (EC50: 8 nM)
Inhibit Orai2 and Orai3 at 10 µM
[214,215,216,217,218,219]
GSK7975A and GSK-5503A Potentially allosteric effect on the selectivity filter of Orai 4 µM Orai2 and Orai3 at 10 µM, L-type Ca2+ (IC50: 8 µM), and TRPV6 channels [219,220]
Synta-66 Binds TM1 and TM3 helices and the extracellular loop segments 26 nM-3 µM Potentiate Orai2 at 10 µM [219,221,222,223,224]
JPIII - 244 nM - [225]
Gd3+ or La3+ Binds extracellular loop of Orai1 200 nM Inhibit Orai2/3 [219,226]
AnCoA4 Binds the C-terminus of Orai1 880 nM - [227]
5J-4 - 10 µM - [228]
STIM1 Inhibitor
ML-9 Inhibit STIM1 puncta formation 10 µM Inhibit Myosin light chain kinase [229]
TRPC3 Inhibitor
Pyr3 Direct binding 0.7 μM - [230]
Pyr10 - 0.72 µM - [218]
TRPC4 Inhibitor
ML-204 - 1–3 μM Inhibit TRPC5 and weakly TRPC6 [231]
HC-070 Direct binding 9.3 nM Inhibit TRPC4 (IC50:46 nM) and
TRPC3 (IC50: 1 µM)
[232,233]
HC-608 (Pico145) - 0.35 nM Inhibit TRPC5 (IC50: 1.3 nM), TRPC1-4 complex (IC50: 0.03 nM) and TRPC1-5 complex (IC50: 0.2 nM) [234]
TRPC5 Inhibitor
AC1903 - 13.6 μM Inhibit TRPC4 (IC50 > 100 µM) [235]
GFB-8438 Direct binding 0.18 µM Inhibit TRPC4 (IC50: 0.29 µM) [236,237]
TRPC6 Inhibitor
SAR7334 - 9.5 nM Inhibit TRPC3 (IC50: 282 nM) and
TRPC7 (IC50: 226 nM)
[238]
SKF-96365 - 10 µM - [239]
GSK2833503 - 3 nM Inhibit TRPC3 (IC50: 21 nM) [240,241]
BI 749327 - 19 nM - [242]
SH045 - 7.9 nM Inhibit TRPC3 (IC50: 282 nM) and
TRPC7 (IC50: 226 nM)
[243]
AM-1473 Direct binding 0.22 nM - [244]

Inhibitors are classified according to their smallest IC50. EC50, half maximal effective concentration; IC50, half maximal inhibitory concentration; -, no data available.