CAS: 1567335-29-8

Cav 2.2 blocker 1 is a hydroxylated flavonol that is an inhibitor of the Cav 2.2 channel. It has been shown to have potent anthelmintic activity in vitro, and it may also have antiangiogenic properties in vivo. Cav 2.2 blocker 1 has been shown to inhibit the proliferation of HL-60 cells by blocking the apoptosis pathway, and it inhibits the invasion of human hepatoma cells in vitro. The structural analysis of Cav 2.2 blocker 1 revealed that this compound binds to group P2 of the ATP binding site on the Cav 2.2 channel, which is located in a hydrophobic pocket formed by three phenylalanine residues at positions 325, 327, and 329 on subunit A (P325A/P327A/P329A). This binding mode is similar to that observed for other inhibitors of the Cav 2.2 channel such as 3-o-caffeoylquinic acid and N

Cav 2.2 blocker 1 is an N-type calcium channel (Cav 2.2; IC50: 1 nM) blocker for the treatment of pain.

Cav 2.2 blocker 1