DASA-58

SKU: orb1223393

Description

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

Key Properties

• CAS Number: 1203494-49-8
• MW: 453.53
• Purity: >98% (HPLC)
• Formula: C₁₉H₂₃N₃O₆S₂
• SMILES: c1(cc(ccc1)S(=O)(=O)N1CCN(CCC1)S(=O)(=O)c1cc2OCCOc2cc1)N
• Target: CDK
• Solubility: DMSO : ≥ 35 mg/mL 77.17 mM

Bioactivity

• In Vitro:
  DASA-58 (15 μM; 2 h) potentiates the antitumor effects of other metabolic stressors. DASA-58 (15 μM; 24 h, 72 h) enhances pyruvate kinase activity in breast cancer cells without a clear effect on proliferation. DASA-58 (30 μM, 60 μM; 0-72 h) enhances extracellular acidification and lactate levels in BCa cell lines and induce extracellular acidification levels in prostate cancer cell lines. DASA-58 (15 μM, 30 μM; 0-72 h) affects respiration levels in BCa cells without an indication of mitochondrial damage. DASA-58 (15 μM; 0-72 h) not rescues TXNIP levels in any combintion and mitochondrial inhibitors enhance PKM2 effects on activating AMPK signaling (T172 phosphorylation of AMPK). DASA-58 (15 μM; 0-72 h) leads to depletion in TXNIP levels independent of AMPK and ER signaling, and not through enhanced proteasomal degradation but rather depleted upstream glycolytic intermediates. Cell Viability Assay Cell line: Five breast cancer cell lines (BCa cells) (MDA MB 231, MDA MB 468, HCC 1443, T47-D, MCF7, LnCap, PC3, and DU145). Concentration: 15 μM. Incubation time: 2 h. Result: Could be exploited by other metabolic stressors. Western blot analysis. Cell line: BCa cells. Concentration: 15 μM. Incubation time: 24 h, 72 h. Result: Showed comparable PKM2 protein levels in five breast cancer cell lines, except HCC1443 cells and MDA MB 468 that showed the highest and lowest PKM2 protein levels, respectively.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

CDK