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DASA-58

DASA-58

产品编号 T6816   CAS 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。

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DASA-58 Chemical Structure
DASA-58, CAS 1203494-49-8
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
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: DASA-58 (T6816)
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纯度: 98.99%
纯度: 96.96%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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)

溶液配制表

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

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TargetMol Library Books参考文献

1. Palsson-McDermott EM, et al. Cell Metab. 2015, 21(1), 65-80. 2. Giannoni E, et al. Oncotarget. 2015, 6(27), 24061-24074.

TargetMol Library Books文献引用

1. Yang L, Zhang J, Hu C, et al.Nuclear translocation of PKM2 mediates keratinocyte metabolic reprogramming in psoriasis.Experimental Dermatology.2023
PKM2 activator 2 Dimethylaminomicheliolide HCl Mitapivat DL-Serine Shikonin Disodium monofluorophosphate TEPP-46 PKM2 inhibitor G

相关化合物库

该产品包含在如下化合物库中:
抗癌细胞代谢库 脂代谢化合物库 经典已知活性库 已知活性化合物库 代谢化合物库 抗代谢疾病化合物库 谷氨酰胺代谢化合物库 铜死亡化合物库 NO PAINS 化合物库 糖代谢化合物库

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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。

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Keywords

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

 

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