VR23

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

VR23  纯度: 98.05%

VR23有效抑制胰蛋白酶样蛋白酶 (IC50=1nM), 胰凝乳蛋白酶样蛋白酶 (IC50=50-100 nM), 和caspase样蛋白酶 (IC50=3 μM)。

VR23

VR23 Chemical Structure

CAS No. : 1624602-30-7

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100 mg ￥5500 In-stock
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VR23 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Peptidomimetic Library
  • Ubiquitination Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

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 & Target

IC50: 1 nM (trypsin-like proteasome), 50-100 nM (chymotrypsin-like proteasome), 3 μM (caspase-like proteasome)
体外研究
(In 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 PS-341. VR23 as a structurally novel proteasome inhibitor with desirable properties as an anticancer agent.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

VR23 shows effective antitumor and antiangiogenic activities in mice.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

477.88

Formula

C19H16ClN5O6S
CAS 号

1624602-30-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL (69.75 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0926 mL 10.4629 mL 20.9258 mL
5 mM 0.4185 mL 2.0926 mL 4.1852 mL
10 mM 0.2093 mL 1.0463 mL 2.0926 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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.

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