Molecular Formula | C19H16ClN5O6S |
Molar Mass | 477.88 |
Solubility | 10 mM in DMSO |
Storage Condition | -20℃ |
In vitro study | VR23 induces accumulation of ubiquitinated proteins 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 | VR23 (30mg/kg, I. p.) showed potent anti-tumor and anti-angiogenic activity in ATH490 athymic mice inoculated with MDA-MB-231 metastatic breast cancer cells. In mice, VR23 also reduced the side effects caused by paclitaxel. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.093 ml | 10.463 ml | 20.926 ml |
5 mM | 0.419 ml | 2.093 ml | 4.185 ml |
10 mM | 0.209 ml | 1.046 ml | 2.093 ml |
5 mM | 0.042 ml | 0.209 ml | 0.419 ml |
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. |