| DASA-58activator of pyruvate kinase M2 (PKM2) |
Sample solution is provided at 25 µL, 10mM.
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| Cas No. | 1203494-49-8 | SDF | Download SDF |
| Chemical Name | 3-((4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)sulfonyl)-1,4-diazepan-1-yl)sulfonyl)aniline | ||
| Canonical SMILES | O=S(N1CCN(S(C2=CC(OCCO3)=C3C=C2)(=O)=O)CCC1)(C4=CC=CC(N)=C4)=O | ||
| Formula | C19H23N3O6S2 | M.Wt | 453.53 |
| Solubility | ≥127.2mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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].
Reference: [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.
