Powder: -20°C for 3 years | In solvent: -80°C for 1 year
VR23 是一种蛋白酶体抑制剂,对胰蛋白酶样蛋白酶体、糜蛋白酶样蛋白酶体和半胱天冬酶样蛋白酶体的 IC50 分别是1 nM、50-100 nM 和3 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 283 | 现货 | ||
5 mg | ¥ 448 | 现货 | ||
10 mg | ¥ 788 | 现货 | ||
25 mg | ¥ 1,480 | 现货 | ||
50 mg | ¥ 2,660 | 现货 | ||
100 mg | ¥ 4,570 | 现货 | ||
200 mg | ¥ 6,390 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 490 | 现货 |
产品描述 | VR23 is a potent proteasome inhibitor. Data shows IC50 =1 nM for trypsin-like proteasomes, IC50=50-100 nM for chymotrypsin-like proteasomes, and IC50=3 μM for caspase-like proteasomes. |
靶点活性 | Trypsin like proteasomes:1 nM, Caspase-like proteasomes:3 μM, Chymotrypsin-like proteasome:50-100 nM |
体外活性 | In 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. [1] |
体内活性 | 在ATH490裸鼠中,接种MDA-MB-231转移性乳腺癌细胞后,VR23(30 mg/kg, i.p.)展现出有效的抗肿瘤和抗血管生成活性。VR23还能减轻紫杉醇在小鼠体内引起的不良反应。[1] |
激酶实验 | Proteasome assay: Exponentially growing cells on a 96-well clustered plate are treated with different concentrations of drugs or left untreated (control) for 6 hours. Proteasomes extracted with 0.5% NP40 buffer are mixed with equal amounts of samples in 100 μL total volume, and then incubated with 25 μmol/L of fluorogenic substrates (LRR- specific for trypsin-like activity, LLE-specific for caspase-like activity, and SUVY-specific for chymotrypsin-like activity) in black-bottom 96-well plates at 37°C. Fluorescence is monitored every 5 minutes at the wavelength of 360 nm (excitation) and 480 nm (emission). |
分子量 | 477.88 |
分子式 | C19H16ClN5O6S |
CAS No. | 1624602-30-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 29 mg/mL (60.7 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0926 mL | 10.4629 mL | 20.9258 mL | 52.3144 mL |
5 mM | 0.4185 mL | 2.0926 mL | 4.1852 mL | 10.4629 mL | |
10 mM | 0.2093 mL | 1.0463 mL | 2.0926 mL | 5.2314 mL | |
20 mM | 0.1046 mL | 0.5231 mL | 1.0463 mL | 2.6157 mL | |
50 mM | 0.0419 mL | 0.2093 mL | 0.4185 mL | 1.0463 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
VR23 1624602-30-7 Apoptosis Proteases/Proteasome Ubiquitination Proteasome Caspase VR-23 inhibit VR 23 Inhibitor inhibitor