DASA-58

DASA-58 is a selective activator of pyruvate kinase M2 (PKM2, AC50 = 38 nM in vitro, EC50 = 19.6 µM in cells). DASA-58 converts PKM2 to a constitutively active enzyme state that is resistant to inhibition by tyrosine-phosphorylated proteins. Through its effects on PKM2, DASA-58 blocks the induction of HIF-1alpha by lipopolysaccharide in bone marrow-derived macrophages, suppressing the expression of several HIF-1alpha-dependent targets, including IL-1beta. It also impairs metastatic dissemination of prostate cancer PCa cells in SCID mice.Formal Name: 3-[[4-[(2,3-dihydro-1,4-benzodioxin-6-yl)sulfonyl]hexahydro-1H-1,4-diazepin-1-yl]sulfonyl]-benzenamine. CAS Number: 1203494-49-8. Synonyms: ML-203, NCGC00185916. Molecular Formula: C19H23N3O6S2. Formula Weight: 453.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 30 mg/ml. lambdamax: 211, 246, 292 nm. SMILES: O=S(N1CCN(S(C2=CC=C(OCCO3)C3=C2)(=O)=O)CCC1)(C4=CC(N)=CC=C4)=O. InChi Code: InChI=1S/C19H23N3O6S2/c20-15-3-1-4-16(13-15)29(23,24)21-7-2-8-22(10-9-21)30(25,26)17-5-6-18-19(14-17)28-12-11-27-18/h1,3-6,13-14H,2,7-12,20H2. InChi Key: GMHIOMMKSMSRLY-UHFFFAOYSA-N.