DASA-58

Synonym(s):3-(4-(2,3-Dihydrobenzo[b][1,4]dioxin-6-ylsulfonyl)-1,4-diazepan-1-ylsulfonyl)aniline;DASA 58;DASA58;N,N′-DiArylSulfonAmide 58;

CAS NO.：1203494-49-8
Empirical Formula: C19H23N3O6S2
Molecular Weight: 453.53
MDL number: MFCD29472280
Update Date: 2026-09-10 08:17:50

What is DASA-58?

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.

Properties of DASA-58

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

Safety information for DASA-58

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H302:Acute toxicity,oral
Precautionary Statement Codes	P280:Wear protective gloves/protective clothing/eye protection/face protection. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for DASA-58

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