Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Gambogic Acid (Guttic Acid) 是来自藤黄树的一种藤黄树脂,抑制 Bcl-XL、Bcl-2、Bcl-W、Bcl-B、Bfl-1和 Mcl-1,IC50分别为 1.47 μM、1.21 μM、2.02 μM、0.66 μM、1.06 μM 和 0.79 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
20 mg | ¥ 570 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 480 | 现货 |
产品描述 | Gambogic Acid (Guttic Acid) ( EC50=0.78-1.64 uM) activates caspases. Gambogic Acid competitively suppresses Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1. The IC50s of Gambogic Acid for Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 are 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 uM, respectively. |
靶点活性 | BCL-B:0.66μM, BCL-W:2.02μM, BCL-XL:1.47μM, BCL2:1.21μM, Bfl-1:1.06μM, MCL1:0.79 μM |
体外活性 | Gambogic Acid is a caged xanthone that is derived from Garcinia hanburyi and functions as a strong apoptotic inducer in many types of cancer cells by inhibiting human Bcl-2 family proteins and activating caspases. Gambogic Acid also blocks Kir2.1 channels with EC50 of ≤ 100 nM.[1] [2] [3] Gambogic Acid significantly inhibits human umbilical vein endothelial cell (HUVEC) proliferation, migration, invasion, tube formation, and micro-vessel growth at nM concentration. [4] |
体内活性 | Gambogic Acid effectively inhibits tumor angiogenesis and suppressed tumor growth with low side effects using metronomic chemotherapy with Gambogic Acid. [4] Gambogic Acid has multiple functional effects including the induction of apoptosis, the inhibition of proliferation and the prevention of cancer metastasis and tumor angiogenesis. [5] In both animal tumor models and Clinicalal trials, Gambogic Acid efficiently inhibits tumor growth with minimal side effects, with little toxicity on immune and hemopoietic systems. Gambogic Acid can produce tissue-specific proteasome inhibition and tumor-specific toxicity. [6] LD50: Mice 45 mg/kg (i.p.). [7] |
激酶实验 | The fluorescence polarization reactions are performed. For Kidetermination, duplicate 200 μL reactions are set up at eight different ATP concentrations from 200 μM (2-fold serial dilutions) in the presence of either DMSO or R406 at 125, 62.5, 31.25, 15.5, or 7.8 nM. At different time points, 20 μL of each reaction is removed and quenched to stop the reaction. For each concentration of R406, the rate of reaction at each concentration of ATP is determined and plotted against the ATP concentration to determine the apparent Km and Vmax (maximal rate). Finally the apparent Km (or apparent Km/Vmax) is plotted against the inhibitor concentration to determine the Ki. All data analysis is performed using Prism and Prism enzyme kinetics programs[1] |
别名 | 藤黄酸, Beta-Guttiferrin, 藤黄酸 A, Guttatic Acid, Guttic Acid |
分子量 | 628.75 |
分子式 | C38H44O8 |
CAS No. | 2752-65-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
DMSO: 47.2 mg/mL (75 mM)
Ethanol: 62.9 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.5905 mL | 7.9523 mL | 15.9046 mL | 39.7614 mL |
5 mM | 0.3181 mL | 1.5905 mL | 3.1809 mL | 7.9523 mL | |
10 mM | 0.159 mL | 0.7952 mL | 1.5905 mL | 3.9761 mL | |
20 mM | 0.0795 mL | 0.3976 mL | 0.7952 mL | 1.9881 mL | |
50 mM | 0.0318 mL | 0.159 mL | 0.3181 mL | 0.7952 mL | |
Ethanol | 100 mM | 0.0159 mL | 0.0795 mL | 0.159 mL | 0.3976 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。
Gambogic Acid 2752-65-0 Apoptosis Autophagy BCL Bcl-2 Family 藤黄酸 β-Guttiferrin b-Guttiferrin Inhibitor Beta-Guttiferrin 藤黄酸 A inhibit Guttatic Acid Guttic Acid inhibitor