biological activity | VR23 is a potent proteome inhibitor that acts on the trypsin-like proteasome, and the caspase-like proteasome have an IC50 of 1 nM,50-100 nM, and 3 μm, respectively. |
Target | TargetValue Trypsin-like protasomes (in Hela cells) 1 nM Chymotrypsin-like protasomes (in Hela cells) 100 nM Caspase-like proteasomes (in Hela cells) 3 μm |
Target | Value |
Trypsin-like proteasomes
(in Hela cells)
| 1 nM |
Chymotrypsin-like proteasomes
(in Hela cells)
| 100 nM |
Caspase-like proteasomes
(in Hela cells)
| 3 μM |
in vitro study | VR23 induces ubiquitinated protein accumulation in HeLa cells. In RPMI 8226 and KAS 6 cells, VR23 inhibited cell growth with an IC50 of 2.94 and 1.46 μm, respectively. VR23 was as effective against bortezomib (BTZ)-sensitive and resistant RPMI 8226 as ANBL6 cells. In the above cells, VR23 showed a synergistic effect on cell growth inhibition when used in combination with bortezomib. Furthermore, VR23 selectively induces cancer cell apoptosis by causing accumulation of ubiquitinated cyclin E. |
in vivo study | in ATH490 athymic mice inoculated with MDA-MB-231 metastatic breast cancer cells, VR23 (30mg/kg, I. p.) exhibits potent anti-tumor and anti-angiogenic activity. In mice, VR23 also reduced the side effects caused by paclitaxel. |