DASA-58

製品コードS7928 バッチS792801

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H23N3O6S2
分子量 453.53 CAS No. 1203494-49-8
Solubility (25°C)* 体外 DMSO 91 mg/mL (200.64 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
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. 
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. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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]

プロトコル(参考用のみ)

キナーゼアッセイ Pyruvate kinase activity
PK activity is measured by a double reactions kinetic assay by lysing cells in 50 mM Tris-HCl pH 7.4, additioned with protease inhibitors and transferred to a TRAP/4 solution (100 mM triethanolamine, 10 mM EDTA, 16 mM MgSO4, pH 7.6) additioned of ADP 100 mM, NADH 10 mM, PEP 40 mM, LDH. The absorbance at 340 nm is monitored over 20 min (ε = 6.22 mM−1 cm−1).
動物実験 動物モデル Male SCID-bg/bg mice bearing PC3 tumors
投薬量 40 μM
投与方法 Drug-treated cells are injected into mice by i.v.

カスタマーフィードバック

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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Chlorpromazine affects glioblastoma bioenergetics by interfering with pyruvate kinase M2 [ Cell Death Dis, 2023, 14(12):821] PubMed: 38092755
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。