WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407205
Description: 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
Chemical Formula: C19H16ClN5O6S
Exact Mass: 477.05098
Molecular Weight: 477.876
Elemental Analysis: C, 47.75; H, 3.37; Cl, 7.42; N, 14.66; O, 20.09; S, 6.71
Synonym: VR23, VR-23, VR 23
IUPAC/Chemical Name: 7-chloro-4-(4-((2,4-dinitrophenyl)sulfonyl)piperazin-1-yl)quinoline
InChi Key: PDQVZPPIHADUOO-UHFFFAOYSA-N
InChi Code: InChI=1S/C19H16ClN5O6S/c20-13-1-3-15-16(11-13)21-6-5-17(15)22-7-9-23(10-8-22)32(30,31)19-4-2-14(24(26)27)12-18(19)25(28)29/h1-6,11-12H,7-10H2
SMILES Code: O=S(N1CCN(C2=CC=NC3=CC(Cl)=CC=C32)CC1)(C4=C(C=C(C=C4)[N+]([O-])=O)[N+]([O-])=O)=O
1: Pundir S, Vu HY, Solomon VR, McClure R, Lee H. VR23: A Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E-Mediated Centrosome Amplification. Cancer Res. 2015 Oct 1;75(19):4164-75. doi:10.1158/0008-5472.CAN-14-3370. Epub 2015 Aug 3. PubMed PMID: 26238784.