VR23 is a potent and selective inhibitor of trypsin-like proteasomes (IC50 = 1 nmol/L), chymotrypsin-like proteasomes (IC50 = 50-100 nmol/L), and caspase-like proteasomes (IC50 = 3 μmol/L). The primary molecular target of VR23 was β2 of the 20S proteasome catalytic subunit. Notably, VR23 was structurally distinct from other known proteasome inhibitors and selectively killed cancer cells by apoptosis, with little effect on noncancerous cells. VR23 was effective in vivo in controlling multiple myelomas and metastatic breast cancer cells, in the latter case also enhancing the antitumor activity of paclitaxel while reducing its side effects.
MedKoo Cat#: 407205
Name: VR23
CAS#: 1624602-30-7
Chemical Formula: C19H16ClN5O6S
Exact Mass: 477.0510
Molecular Weight: 477.88
Elemental Analysis: C, 47.75; H, 3.37; Cl, 7.42; N, 14.66; O, 20.09; S, 6.71
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 21.6 | 45.22 | |
| DMF | 2.0 | 4.19 | |
| DMF:PBS (pH 7.2) (1:2) | 0.3 | 0.63 | |
| Water | 5.0 | 10.46 |
The following data is based on the product molecular weight 477.88 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
