DASA-58

SKU: orb1300440

Description

DASA-58 is a potent and selective small molecule activator of the Pyruvate Kinase M2 (PKM2) isoform. Its application in research includes studying cancer metabolism, where PKM2 modulation is explored in both cellular and animal models to investigate tumor growth and metabolic reprogramming.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1203494-49-8
• MW: 453.53
• Purity: 99.28% (May vary between batches)
• Formula: C₁₉H₂₃N₃O₆S₂
• SMILES: Nc1cccc(c1)S(=O)(=O)N1CCCN(CC1)S(=O)(=O)c1ccc2OCCOc2c1
• Target: PKM
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.28 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:125.5 mg/mL (276.72 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• In Vivo:
  DASA-58 (40 μM) affects EMT of prostate cancers and tumor dissemination in SCID mice.
• 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. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PKM2, Pyruvate Kinase, pyruvate kinase M2, TXNIP, inhibit, Inhibitor, glycolysis, AMPK, cancer metabolism, breast cancer, DASA 58, DASA58, DASA-58

Compound Identifiers

PubChem CID

44543605