VR-23

Research use only, not for human use.

A potent inhibitor of trypsin-like proteasome (IC50=1 nM), chymotrypsin-like proteasome (IC50=50-100 nM) and caspase-like proteasome (IC50=3 uM).

A potent inhibitor of trypsin-like proteasome (IC50=1 nM), chymotrypsin-like proteasome (IC50=50-100 nM) and caspase-like proteasome (IC50=3 uM); targets the β2 of the 20S proteasome catalytic subunit and structurally distinct from other known proteasome inhibitors and selectively kills cancer cells by apoptosis, with little effect on noncancerous cells.

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 PS-341. VR23 as a structurally novel proteasome inhibitor with desirable properties as an anticancer agent.

VR23 shows effective antitumor and antiangiogenic activities in mice.

VR23

Proteasome/Ubiquitin

Proteasome

Caspase-likeproteasomes|Chymotrypsin-likeproteasomes|Trypsin-likeproteasomes

Metabolic Disease

——

1624602-30-7

477.8782

C19H16ClN5O6S

>98% (HPLC)

10 mM in DMSO

O=S(N1CCN(C2=CC=NC3=CC(Cl)=CC=C32)CC1)(C4=C(C=C(C=C4)[N+]([O-])=O)[N+]([O-])=O)=O

Quinoline, 7-chloro-4-[4-[(2,4-dinitrophenyl)sulfonyl]-1-piperazinyl]-

(-20℃)

With Ice Pack

≥ 2 years