| Identification | Back Directory | [Name]
DASA-58 | [CAS]
1203494-49-8 | [Synonyms]
DASA-58
CS-1563
DASA58; DASA 58
3-[[4-[(2,3-Dihydro-1,4-benzodioxin-6-yl)sulfonyl]hexahydro-1H-1,4-diazepin-1-yl]sulfonyl]benzenamine
Benzenamine, 3-[[4-[(2,3-dihydro-1,4-benzodioxin-6-yl)sulfonyl]hexahydro-1H-1,4-diazepin-1-yl]sulfonyl]- | [Molecular Formula]
C19H23N3O6S2 | [MDL Number]
MFCD29472280 | [MOL File]
1203494-49-8.mol | [Molecular Weight]
453.53 |
| Chemical Properties | Back Directory | [Boiling point ]
681.5±65.0 °C(Predicted) | [density ]
1.453±0.06 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Inert atmosphere,Store in freezer, under -20°C | [solubility ]
insoluble in EtOH; insoluble in H2O; ≥127.2 mg/mL in DMSO | [form ]
solid | [pka]
3.35±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
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-1α by lipopolysaccharide in bone marrow-derived macrophages, suppressing the expression of several HIF-1α-dependent targets, including IL-1β. It also impairs metastatic dissemination of prostate cancer PCa cells in SCID mice. | [Definition]
ChEBI: 3-[[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-1,4-diazepan-1-yl]sulfonyl]aniline is a member of benzenes and a sulfonamide. | [References]
[1]. anastasiou d, yu y, israelsen wj, et al. pyruvate kinase m2 activators promote tetramer formation and suppress tumorigenesis. nature chemical biology, 2012, 8(10): 839-847. |
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