DASA-58 NEW
| Price | $37 | $64 | $97 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: DASA-58 | CAS No.: 1203494-49-8 |
| Purity: 99.28% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | DASA-58 |
| Description | DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator. |
| Kinase Assay | 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. |
| In vitro | 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] |
| In vivo | DASA-58 (40 μM) affects EMT of prostate cancers and tumor dissemination in SCID mice. [2] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 84 mg/mL (185.2 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) |
| Keywords | inhibit | Inhibitor | glycolysis | TXNIP | DASA 58 | cancer metabolism | DASA58 | Pyruvate Kinase | pyruvate kinase M2 | DASA-58 | breast cancer | AMPK |
| Inhibitors Related | DL-Serine | PKM2-IN-1 | PKR-IN-2 | Disodium monofluorophosphate | Shikonin | Mitapivat | PKM2 inhibitor G | Dimethylaminomicheliolide HCl | TEPP-46 | PKM2 activator 5 | PKM2 activator 2 |
| Related Compound Libraries | Glycolysis Compound Library | Glycometabolism Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Metabolism Compound Library | NO PAINS Compound Library | Lipid Metabolism Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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