货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T93484-1ml促销	10mM in DMSO	￥588.00 ￥529.00 T93484-1ml ￥529.00 现货	10 10	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T93484-1ml促销

10mM in DMSO

￥588.00 ￥529.00

产品描述：

蛋白酶体抑制剂;Proteasome Inhibitors;;InformationVR23 VR23 is a potent proteasome inhibitor with IC50 of 1 nM, 50-100 nM, and 3 μM for trypsin-like proteasomes, chymotrypsin-like proteasomes, and caspase-like proteasomes, respectively.TargetsTrypsin-like proteasomes (in Hela cells); Chymotrypsin-like proteasomes (in Hela cells); Caspase-like proteasomes (in Hela cells) 1 nM; 100 nM; 3 μMIn vitroIn HeLa cells, VR23 induces ubiquitinated proteins accumulation. In RPMI 8226 and KAS 6 cells, VR23 inhibits cell growth with IC50 of 2.94 and 1.46 μM, respectively. VR23 is also equally effective on both bortezomib (BTZ)-sensitive and -resistant RPMI 8226 and ANBL6 cells cells. When used in combination of bortezomib in the cells above, VR23 shows synergistic effects on cell growth inhibition. In addition, VR23 selectively induces cancer cell apoptosis by causing the accumulation of ubiquitinated cyclin E.In vivoIn ATH490 athymic mice engrafted with MDA-MB-231 metastatic breast cancer cells, VR23 (30mg/kg, i.p.) shows effective antitumor and antiangiogenic activities. VR23 also reduces adverse effects caused by paclitaxel in mice.Cell Research(from reference)Cell lines：RPMI 8226, KAS 6, 184B5, and MCF10A cells; bortezomib-resistant RPMI 8226 cells and bortezomib-resistant ANBL6 cells Concentrations：~20 μM

靶点：

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

体内研究：

VR23 在小鼠体内显示出有效的抗肿瘤和抗血管生成活性。

参考文献：

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.

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.093 ml	10.463 ml	20.926 ml
5 mM	0.419 ml	2.093 ml	4.185 ml
10 mM	0.209 ml	1.046 ml	2.093 ml
50 mM	0.042 ml	0.209 ml	0.419 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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