化合物 DASA58|T6816|TargetMol

DASA-58
1203494-49-8

￥301 1mg 起订

￥453 2mg 起订

￥872 5mg 起订

上海更新日期：2024-09-30

TargetMol中国（陶术生物）

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联系人：邵小姐

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邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 DASA58

英文名称：: DASA-58

CAS号：: 1203494-49-8

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.28%

产品类别：: 抑制剂

货号：: T6816

Product Introduction

Bioactivity

名称	DASA-58
描述	DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.
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.
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]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 84 mg/mL (185.2 mM) H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字	inhibit \| Inhibitor \| glycolysis \| TXNIP \| DASA 58 \| cancer metabolism \| DASA58 \| Pyruvate Kinase \| pyruvate kinase M2 \| DASA-58 \| breast cancer \| AMPK
相关产品	PKM2 activator 2 \| Dimethylaminomicheliolide HCl \| PKM2 inhibitor G \| PKM2-IN-1 \| PKR-IN-2 \| DL-Serine \| PKM2 activator 5 \| Mitapivat \| Shikonin \| Disodium monofluorophosphate \| TEPP-46
相关库	脂代谢化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| 抗癌细胞代谢库 \| 代谢化合物库 \| 激酶抑制剂库 \| 糖代谢化合物库 \| 糖酵解化合物库 \| 抗代谢疾病化合物库 \| 铜死亡化合物库

DASA-58|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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