1624602-30-7

1624602-30-7 structure

Name: VR23
Chemical Name: 7-Chloro-4-[4-[(2,4-dinitrophenyl)sulfonyl]-1-piperazinyl]quinoline
CAS Number: 1624602-30-7
Molecular Formula: C₁₉H₁₆ClN₅O₆S
Molecular Weight: 477.878
Catalog: Signaling Pathways Metabolic Enzyme/Protease Proteasome
Create Date: 2018-12-10 19:57:54
Modify Date: 2024-01-03 17:36:45
VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3 μM).IC50 value: 1 nM (trypsin-like proteasome), 50-100 nM(chymotrypsin-like proteasome), 3 μM (caspase-like proteasome)Target: proteasomein vitro: 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 bortezomib. VR23 as a structurally novel proteasome inhibitor with desirable properties as an anticancer agent.in vivo: VR23 shows effective antitumor and antiangiogenic activities in mice.

Name	7-Chloro-4-[4-[(2,4-dinitrophenyl)sulfonyl]-1-piperazinyl]quinoline
Synonyms	7-Chloro-4-{4-[(2,4-dinitrophenyl)sulfonyl]-1-piperazinyl}quinoline Quinoline, 7-chloro-4-[4-[(2,4-dinitrophenyl)sulfonyl]-1-piperazinyl]- VR23

Description	VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3 μM).IC50 value: 1 nM (trypsin-like proteasome), 50-100 nM(chymotrypsin-like proteasome), 3 μM (caspase-like proteasome)Target: proteasomein vitro: 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 bortezomib. VR23 as a structurally novel proteasome inhibitor with desirable properties as an anticancer agent.in vivo: VR23 shows effective antitumor and antiangiogenic activities in mice.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome Research Areas >> Metabolic Disease
References	[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. [2]. Lee Hoyun, et al. Preparation of quinoline sulfonyl derivatives for the treatment of cancer. From PCT Int. Appl. (2014), WO 2014134705 A1 20140912.