VR23 

VR23 is a small molecule that potently inhibits the activities of trypsin-like proteasomes (IC₅₀=1 nM), chymotrypsin-like proteasomes (IC₅₀=50-100 nM), and caspase-like proteasomes (IC₅₀=3 μM).

IC50: 1 nM (trypsin-like proteasome), 50-100 nM (chymotrypsin-like proteasome), 3 μM (caspase-like proteasome)

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

VR23 shows effective antitumor and antiangiogenic activities in mice.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

477.88

Solid

C₁₉H₁₆ClN₅O₆S

1624602-30-7

O=S(N1CCN(C2=CC=NC3=CC(Cl)=CC=C23)CC1)(C4=CC=C([N+]([O-])=O)C=C4[N+]([O-])=O)=O

Room temperature in continental US; may vary elsewhere.

• [1]. Pundir S, et al. VR23: A Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E-Mediated Centrosome Amplification. Cancer Res. 2015 Oct 1;75(19):4164-4175.  [Content Brief]

  [2]. Lee Hoyun, et al. Preparation of quinoline sulfonyl derivatives for the treatment of cancer. From PCT Int. Appl. (2014), WO 2014134705 A1 20140912.