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DASA-58

Catalog No. T6816   CAS 1203494-49-8

DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.

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DASA-58 Chemical Structure
DASA-58, CAS 1203494-49-8
Pack Size Availability Price/USD Quantity
2 mg In stock $ 37.00
5 mg In stock $ 64.00
10 mg In stock $ 97.00
25 mg In stock $ 198.00
50 mg In stock $ 345.00
100 mg In stock $ 547.00
1 mL * 10 mM (in DMSO) In stock $ 70.00
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Purity: 98.99%
Purity: 96.96%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.
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]
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.
Molecular Weight 453.53
Formula C19H23N3O6S2
CAS No. 1203494-49-8

Storage

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

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)

TargetMolReferences and Literature

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

TargetMolCitations

1. Yang L, Zhang J, Hu C, et al.Nuclear translocation of PKM2 mediates keratinocyte metabolic reprogramming in psoriasis.Experimental Dermatology.2023

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compounds Library Max Lipid Metabolism Compound Library Glycometabolism Compound Library NO PAINS Compound Library Metabolism Compound Library Target-Focused Phenotypic Screening Library Glycolysis Compound Library Glutamine Metabolism Compound Library Anti-Cancer Metabolism Compound Library Cuproptosis Compound Library

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Related compounds with same targets
PKM2 activator 2 Dimethylaminomicheliolide HCl Mitapivat DL-Serine Shikonin Disodium monofluorophosphate TEPP-46 PKR-IN-2

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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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