Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DASA58 是一种有效的丙酮酸激酶M2 (PKM2) 活化剂,其中AC90=680 nM,AC50=38 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 301 | 现货 | ||
2 mg | ¥ 453 | 现货 | ||
5 mg | ¥ 872 | 现货 | ||
10 mg | ¥ 1,580 | 现货 | ||
25 mg | ¥ 2,930 | 现货 | ||
50 mg | ¥ 4,330 | 现货 | ||
100 mg | ¥ 6,170 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 959 | 现货 |
产品描述 | DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator. |
体外活性 | DASA-58 inhibits LPS-induced Hif-1α and IL-1β, as well as the expression of a range of other Hif-1α-dependent genes in primary BMDMs, and also inhibits glycolysis and the accumulation of succinate in LPS-activated macrophages. [1] In PC3 cells, DASA-58 impairs stromal-induced EMT program by restoring PK activity and abrogating the nuclear translocation of PKM2, as well as its association with HIF-1α. DASA-58 also dramatically reduces (~6-fold) CAFs-induced lung metastases formation in PC3 cells. [2] |
体内活性 | DASA-58 (40 μM) affects EMT of prostate cancers and tumor dissemination in SCID mice. [2] |
激酶实验 | CDK kinase assay: Kinase assays are performed in 96-well polypropylene plates. Each reaction contained 2 μg of histone H1 at a final concentration of 10 μM [γ-33P]ATP (0.2 μCi/well; approximately twice the experimentally determined Km), 10 mM MgCl2, 1 mM DTT, 0.01% Triton X-100, and 10% glycerol in a 40 μL volume. The reaction is initiated with the addition of 20 μL enzyme (6 ng cdk2/well resulting in a final concentration of 1.6 nM), which is previously diluted 1:50–1:200 in the same buffer, and allowed to proceed for 1 h at room temperature. Reaction is stopped by the addition of 0.01 mL 10% phosphoric acid, and 25 μL of reaction mixture is transferred to P30 phosphocellulose filter mat paper. The filter mat is washed three times with 1.0% phosphoric acid, air dried, and then counted for radioactivity in a liquid scintillation counter. The cdk4 kinase assay for cyclin D1-cdk4 is carried out in a polypropylene 96-well microtiter plate format measuring the incorporation of radioactive phosphate into GST-Rb. Purified cyclin D1-cdk4 is incubated with 1 μg GST-Rb in 20 mM HEPES (pH 7.5) in the presence of 10 mM MgCl2, 1 mM DTT, 0.01% Triton X-100, and 10% glycerol. The final cdk4 concentration is 10 ng/well, or 1.6 nM. Kinase reaction is initiated by the addition of ATP at a final concentration of 10 μM ATP (twice the experimentally determined Km) and [γ-33P]ATP (1.0 μCi per well) in a 60-μL volume and allowed to proceed at room temperature for 1 h. Reaction is stopped by the addition of 0.01 ml 10% phosphoric acid, and 25 μL of reaction mixture is transferred to P30 phosphocellulose filter mat paper. The filter mat is treated as for Cdk1/Cdk2 assays. |
分子量 | 453.53 |
分子式 | C19H23N3O6S2 |
CAS No. | 1203494-49-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 84 mg/mL (185.2 mM)
H2O: < 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 | 2.2049 mL | 11.0246 mL | 22.0493 mL | 55.1231 mL |
5 mM | 0.441 mL | 2.2049 mL | 4.4099 mL | 11.0246 mL | |
10 mM | 0.2205 mL | 1.1025 mL | 2.2049 mL | 5.5123 mL | |
20 mM | 0.1102 mL | 0.5512 mL | 1.1025 mL | 2.7562 mL | |
50 mM | 0.0441 mL | 0.2205 mL | 0.441 mL | 1.1025 mL | |
100 mM | 0.022 mL | 0.1102 mL | 0.2205 mL | 0.5512 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。
DASA-58 1203494-49-8 Metabolism PKM inhibit Inhibitor glycolysis TXNIP DASA 58 cancer metabolism DASA58 Pyruvate Kinase pyruvate kinase M2 breast cancer AMPK inhibitor