CM-4620

1713240-67-5

C19H11ClF3N3O3

DMSO : >= 100 mg/mL (237.10 mM); H2O : < 0.1 mg/mL (insoluble)

Membrane Transporter/Ion Channel

CM-4620 is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC₅₀s of 119 nM, 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively. IC50 & Target: IC50: 119 nM (Orai 1/STIM1), 895 nM (Orai 1/STIM1)^[1]. In Vitro: It is determined that CM-4620 (compound 1) inhibits Orai 1/STIM1 channels with an IC₅₀ of 119 nM, and Orai2/STIM1 channels with an IC₅₀ of 895 nM. It 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 gamma: 138 nM, IL-4: 879 nM, IL-6: 135 nM, IL-1beta: 240 nM, IL-10: 303 nM, TNFalpha: 225 nM, IL-2: 59 nM, IL-17 120 nM)^[1]. In Vivo: Mouse PACs are treated with CRAC inhibitors CM-4620 or GSK-7975A 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 controllevels upon treatment with 700 nM of inhibitor. CM-4620 blocks 100% of reuptake at 10 mM^[1].