DASA-58

A selective PKM2 activator

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货号: ajci10018
CAS: 1203494-49-8
别名: 3-[[4-[(2,3-二氢-1,4-苯并二恶英-6-基)磺酰基]六氢-1H-1,4-二氮杂卓-1-基]磺酰基]苯胺
分子式: C19H23N3O6S2
分子量: 453.53
纯度: >98%
溶解度: ≥ 127.2mg/mL in DMSO
储存: Store at -20°C
库存: 现货

Background

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.