DASA-58

Catalog No.S7928 Batch:S792801

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Technical Data

Formula

C19H23N3O6S2
Molecular Weight 453.53 CAS No. 1203494-49-8
Solubility (25°C)* In vitro DMSO 91 mg/mL (200.64 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.
Targets
PKM2 [1]
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]

Protocol (from reference)

Animal Study:[2]
  • Animal Models

    Male SCID-bg/bg mice bearing PC3 tumors

  • Dosages

    40 μM

  • Administration

    Drug-treated cells are injected into mice by i.v.

Customer Product Validation

Data from [Data independently produced by , , J Mol Cell Biol, 2018, doi:10.1093/jmcb/mjy065]

Selleck's DASA-58 has been cited by 12 publications

Lactylation of PKM2 Suppresses Inflammatory Metabolic Adaptation in Pro-inflammatory Macrophages [ Int J Biol Sci, 2022, 18(16):6210-6225] PubMed: 36439872
PKM2 Modulation in Head and Neck Squamous Cell Carcinoma [ Int J Mol Sci, 2022, 23(2)775] PubMed: 35054968
PDGF-BB/PDGFRβ promotes epithelial-mesenchymal transition by affecting PI3K/AKT/mTOR-driven aerobic glycolysis in Wilms' tumor G401 cells [ Cell Biol Int, 2022, 10.1002/cbin.11780] PubMed: 35165984
Aerobic glycolysis supports hepatitis B virus protein synthesis through interaction between viral surface antigen and pyruvate kinase isoform M2 [ PLoS Pathog, 2021, 17(3):e1008866] PubMed: 33720996
Shikonin alleviates choroidal neovascularization by inhibiting proangiogenic factor production from infiltrating macrophages [ Exp Eye Res, 2021, 213:108823] PubMed: 34752817
Simvastatin re-sensitizes hepatocellular carcinoma cells to sorafenib by inhibiting HIF-1α/PPAR-γ/PKM2-mediated glycolysis. [ J Exp Clin Cancer Res, 2020, 39(1):24] PubMed: 32000827
Pyruvate Kinase M2 Promotes the Activation of Dendritic Cells by Enhancing IL-12p35 Expression [ Cell Rep, 2020, 26;31(8):107690] PubMed: 32460017
PKM2 regulates angiogenesis of VR-EPCs through modulating glycolysis, mitochondrial fission, and fusion. [ J Cell Physiol, 2020, 10.1002/jcp.29549] PubMed: 32017072
PKM2 suppresses osteogenesis and facilitates adipogenesis by regulating β-catenin signaling and mitochondrial fusion and fission. [ Aging (Albany NY), 2020, 12(4):3976-3992] PubMed: 32096765
Interrogation of kinase genetic interactions provides a global view of PAK1-mediated signal transduction pathways [ J Biol Chem, 2020, jbc.RA120.014831] PubMed: 33060198

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.