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DASA-58

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产品编号 T6816Cas号 1203494-49-8

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。

DASA-58
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DASA-58

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纯度: 99.28%
产品编号 T6816Cas号 1203494-49-8

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。

规格价格库存数量
1 mg
¥ 301
现货
2 mg
¥ 453
现货
5 mg
¥ 872
现货
10 mg
¥ 1,580
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25 mg
¥ 2,930
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50 mg
¥ 4,330
现货
100 mg
¥ 6,170
现货
1 mL x 10 mM (in DMSO)
¥ 959
现货
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纯度:99.28%
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产品介绍

生物活性
产品描述
DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.
体外活性
DASA-58在抑制LPS诱导的Hif-1α和IL-1β表达,以及一系列其他依赖Hif-1α的基因在初代BMDMs中的表达方面发挥作用,并且还能抑制LPS激活的巨噬细胞中的糖酵解过程和琥珀酸的积累。[1] 在PC3细胞中,DASA-58通过恢复PK活性和消除PKM2的核内转移及其与HIF-1α的关联,破坏了由基质诱导的EMT程序。同时,DASA-58还显著减少(约6倍)CAF诱导的PC3细胞肺转移瘤的形成。[2]
体内活性
DASA-58 (40 μM) 对前列腺癌的上皮-间质转化(EMT)及在SCID小鼠中的肿瘤扩散产生影响。[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.
化学信息
分子量453.53
分子式C19H23N3O6S2
CAS No.1203494-49-8
SmilesNc1cccc(c1)S(=O)(=O)N1CCCN(CC1)S(=O)(=O)c1ccc2OCCOc2c1
密度1.453 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 84 mg/mL (185.21 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.2049 mL11.0246 mL22.0493 mL110.2463 mL
5 mM0.4410 mL2.2049 mL4.4099 mL22.0493 mL
10 mM0.2205 mL1.1025 mL2.2049 mL11.0246 mL
20 mM0.1102 mL0.5512 mL1.1025 mL5.5123 mL
50 mM0.0441 mL0.2205 mL0.4410 mL2.2049 mL
100 mM0.0220 mL0.1102 mL0.2205 mL1.1025 mL

SCI 文献

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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