| Description | PKM2 activator 2 is a pyruvate kinase M2 (PKM2) activator with an AC 50 value of 66 nM.PKM2 activator 2 has anti-tumor proliferative properties and attenuates the Warburg effect by normalizing cellular glycolytic metabolism through activation of PKM2. |
| In vitro | PKM2 activator 2 (compound 28) is a highly potent activator, activates pyruvate kinase with an AC50 value of 66 nM in the luciferase-coupled assay.[1] |
| Cell experiments | 在 THP-1 细胞中，使用WB检测抑制或激活 PKM2 后 p-STAT3 的表达情况，用 PKM2-IN-1 (T4170, 10 μM) 和 PKM2 activator 2 (T62758, 100 nM) 处理 48 h。 |
| Target activity | PKM2:66 nM (EC50) |
| molecular weight | 452.49 |
| Molecular formula | C20H18F2N2O4S2 |
| CAS | 1186660-06-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 4.5 mg/mL (9.9 mM), Sonication and heating to 60℃ are recommended. |
| References | 1. Boxer MB, et al. Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase. J Med Chem. 2010;53(3):1048-1055. |