VR23有效抑制胰蛋白酶樣蛋白酶 (IC50=1nM), 胰凝乳蛋白酶樣蛋白酶 (IC50 =50-100 nM), 和caspase樣蛋白酶 (IC50 =3μM)。
VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3 μM).
IC50 value: 1 nM (trypsin-like proteasome), 50-100 nM(chymotrypsin-like proteasome), 3 μM (caspase-like proteasome)
Target: proteasome
in vitro: VR23 is a novel proteasome inhibitor targeting β2 of the 20S proteasome subunit. VR23 produces a synergistic effect in killing multiple myeloma cells, including those that were resistant to bortezomib. VR23 as a structurally novel proteasome inhibitor with desirable properties as an anticancer agent.
in vivo: VR23 shows effective antitumor and antiangiogenic activities in mice.