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Catalog No.
activator of pyruvate kinase M2 (PKM2)
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DASA-58 is an selective activator of pyruvate kinase M2 (PKM2) with an AC90 value of 680 nM, and an AC50 value of 38 nM [1].

In cancer, the altered glucose metabolism can be influenced by the regulatory properties of PKM2. The interaction between PKM2 and phosphotyrosine-containing proteins results in the inhibition of enzyme activity and hence more glycolytic metabolites [1].

In A549-PKM1/kd and A549-PKM2/kd cells, Flag-PKM1 and Flag-PKM2 were expressed, respectively. Endogenous PKM2 was knockdowned. Treatment with DMSO resulted in 233±27% more pyruvate kinase activity in lysates from A549-PKM1/kd cells than that in lysates from A549-PKM2/kd cells. Treatment with DASA-58 did not increase the pyruvate kinase activity in A549-PKM1/kd cells, but it resulted in a 248 ±21% pyruvate kinase activity increase in the lysate of A549-PKM2/kd cells. In cells, 0-100 μM of DASA-58 dose-dependently activated PKM2 with an EC50 value of 19.6 μM [1].

TEPP-46 is another PKM2 activator. In A549 xenograft tumors, TEPP-46 at an acute oral-dose of 150 mg/kg resulted in the maximal activation of PKM2. In mice bearing H1299 xenograft tumors, treatment with TEPP-46 at a 5-day repeat-dose of 50 mg/kg twice daily made tumors harbor exclusively tetrameric PKM2. In xenografts from vehicle-treated mice, little tetrameric PKM2 was found [1].

[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.1203494-49-8
Solubilityinsoluble in EtOH; insoluble in H2O; ≥127.2 mg/mL in DMSO
Chemical Name3-((4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)sulfonyl)-1,4-diazepan-1-yl)sulfonyl)aniline
SDFDownload SDF
Canonical SMILESO=S(N1CCN(S(C2=CC(OCCO3)=C3C=C2)(=O)=O)CCC1)(C4=CC=CC(N)=C4)=O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

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