Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MDK83190 (Apoptosis Activator 2) 是一种细胞凋亡激活剂,可诱导 caspase-3 激活、Apaf-1 寡聚化、PARP 切割和 DNA 片段化。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 463 | 现货 | ||
10 mg | ¥ 731 | 现货 | ||
50 mg | ¥ 1,492 | 现货 | ||
100 mg | ¥ 2,379 | 现货 | ||
200 mg | ¥ 3,569 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 522 | 现货 |
产品描述 | MDK83190 (Apoptosis Activator 2) is a potent apoptosis activator, induceing caspase-3 activation, PARP cleavage, and DNA fragmentation . |
靶点活性 | Leukemia origin cells:4-9 uM (IC50) |
体外活性 | Apoptosis Activator 2 (20 μM) at the reduced cyto c concentration increases the fraction of Apaf-1 in the apoptosome by 1.5-fold to 33%. Apoptosis Activator 2 increases the extent of caspase-3 activation at the reduced level of cyto c and caspase-3 activation by 4-fold. Apoptosis Activator 2 strongly indues caspase-3 activation, PARP cleavage, and DNA fragmentation, and finally killing cells with an IC50 of 4 μM. Apoptosis Activator 2 induces apoptosis of PBL, HUVEC, Jurkat, Molt-4, CCRF-CEM, BT-549, MDA-MB-468 and NCI-H23 with of IC50 of 50 μM, 43 μM, 4 μM, 6 μM, 9 μM, 20 μM, 44 μM and 35 μM. Apoptosis Activator 2 exerts a cytostatic effect on the majority of tumor cell lines tested, inhibiting cell growth by 50-100% at 10 μM in 40 of 48 cell lines tested. [1] Apoptosis Activator 2 induces cell death by triggering apoptosome formation. The level of En1 expression does not have a significant influence on the survival rates of Ventral midbrain cultures for Apoptosis Activator 2 (-8.1 ± 6.0%). Survival rate is not significantly altered if the other three reagents are employed (-10.7 ± 4.7%) for Apoptosis Activator 2. [2] Apoptosis activator 2 (10 μM) induces apoptosis in AGS cells as evaluated by apoptotic DNA ladder and Tunel assay. Apoptosis activator 2 (10 μM) enhances the induction of apoptosis by anti TROP2 conjugated liposomes. [3] Cyclohexamide (10 μg/mL) or zVAD (50 μM) significantly protects against Apoptosis Activator 2 toxicity in neuroneal cultures. Apoptosis activator 2 (3 μM) results in numerous neurones with pyknotic nuclei suggestive of cell death involving apoptosis. DHT (10 nM) or E2 (10 nM) significantly protects against Apoptosis Activator 2 toxicity in neuroneal cultures. [4] |
激酶实验 | Cell-Free Apoptosis Assay: HeLa cell cytoplasmic extracts are prepared according to previously published reports. Apoptosis Activator 2 in DMSO are distributed into 96-well microtiter plates at a final concentration of 1 mM (final DMSO concentration is 1% vol/vol). To each well is added 250 μg of total protein from cytoplasmic extracts in HEB buffer (50 mM Hepes, pH 7.4/50 mM KCl/5 mM EGTA/2 mM MgCl), with 2 mM DTT, 2 μM cyto c, and 0.5 μM DEVD-AFC (Asp-Glu-Val-Asp-7-amino-4-trifluoromethylcoumarin) substrate in a total of 150 μL. Plates are incubated at 37 ℃, and fluorescence is read in a LJL Biosystems plate reader at 10-min intervals. |
细胞实验 | All viable cells within the defined field of a microscope reticle grid are counted using a manual mechanical counter by an experimenter blinded to condition. Cells are scored viable on the basis of both positive staining with the vital dye calcein acetoxymethyl ester and the morphological criterion of a smooth, spherical soma. Counts of viable cells are made in four non-overlapping fields per culture well with each condition represented by 3 separate wells. The number of viable cells counts per well for vehicle-treated control conditions ranged from 100-200. All experiments are repeated in at least 3 independent culture preparations. Raw cell count data are statistically analyzed with one-way ANOVA, followed by between group comparisons using the Fisher LSD test (significance indicated by P < 0.05). Cell viability is presented graphically as a percentage of live cells in the vehicle-treated control condition.(Only for Reference) |
别名 | Apoptosis Activator 2 |
分子量 | 306.14 |
分子式 | C15H9Cl2NO2 |
CAS No. | 79183-19-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30.6 mg/mL (100 mM)
Ethanol: 1.5 mg/mL (5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 3.2665 mL | 16.3324 mL | 32.6648 mL | 81.662 mL |
5 mM | 0.6533 mL | 3.2665 mL | 6.533 mL | 16.3324 mL | |
DMSO | 10 mM | 0.3266 mL | 1.6332 mL | 3.2665 mL | 8.1662 mL |
20 mM | 0.1633 mL | 0.8166 mL | 1.6332 mL | 4.0831 mL | |
50 mM | 0.0653 mL | 0.3266 mL | 0.6533 mL | 1.6332 mL | |
100 mM | 0.0327 mL | 0.1633 mL | 0.3266 mL | 0.8166 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。
MDK83190 79183-19-0 Apoptosis Proteases/Proteasome Caspase Apoptosis Activator 2 Inhibitor MDK-83190 inhibit MDK 83190 inhibitor