DASA-58 (ML203) is a potent and selective Pyruvate kinase M2 (PKM2) activator with EC50 ~38 nM. It can stabilize pyruvate kinase subunit interactions, promote PKM2 tetramer formation and prevent inhibition by phosphotyrosine signaling. It can alter metabolism in cultured cells, and inhibit xenograft tumor growth in vivo. 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 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. It also dramatically reduces (~6-fold) CAFs-induced lung metastases formation in PC3 cells.
CAS Number: 1203494-49-8
Molecular Weight: 453.53
Chemical Name: 3-((4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)sulfonyl)-1,4-diazepan-1-yl)sulfonyl)aniline
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
DASA-58 was used at 1-10 µM final concentration in various assays.
DASA-58 (40 μM) treated cells are injected into male SCID-bg/bg mice bearing PC3 tumors by IV.
- Anastasiou D, et al. Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis. (2012) Nat Chem Biol. 8(10):839-47.
- Palsson-McDermott EM, et al. Pyruvate kinase M2 regulates Hif-1α activity and IL-1β induction and is a critical determinant of the warburg effect in LPS-activated macrophages. (2015) Cell Metab. 21(1):65-80.
- Giannoni E, et al. Targeting stromal-induced pyruvate kinase M2 nuclear translocation impairs oxphos and prostate cancer metastatic spread. (2015) Oncotarget. 6(27):24061-74.
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