A selective activator of PKM2 (AC50 = 38 nM in vitro

DASA-58 – 10 mg

Brand:
Cayman
CAS:
1203494-49-8
Storage:
-20
UN-No:
Non-Hazardous - /

DASA-58 is a selective activator of pyruvate kinase M2 (PKM2; AC50 = 38 nM in vitro, EC50 = 19.6 µM in cells).{21504} DASA-58 converts PKM2 to a constitutively active enzyme state that is resistant to inhibition by tyrosine-phosphorylated proteins.{21504} 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.{31878} It also impairs metastatic dissemination of prostate cancer PCa cells in SCID mice.{31877}  

 

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Description

A selective activator of PKM2 (AC50 = 38 nM in vitro, EC50 = 19.6 µM in cells); converts PKM2 to a constitutively active enzyme state that is resistant to inhibition by tyrosine-phosphorylated proteins

Formal name: 3-[[4-[(2,3-dihydro-1,4-benzodioxin-6-yl)sulfonyl]hexahydro-1H-1,4-diazepin-1-yl]sulfonyl]-benzenamine

Synonyms:  ML-203|NCGC00185916

Molecular weight: 453.5

CAS: 1203494-49-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Activators|Kinases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling

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