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DASA-58 is a potent activator of pyruvate kinase M2 (PKM2) with an AC90 of 680 nM, and an AC50 of 38 nM.
| Molecular Weight | 453.53 |
| CAS Number | 1203494-49-8 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 35 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Scott M Seki, et al. Modulation of PKM activity affects the differentiation of T H 17 cells
| Related Pyruvate Kinase Products |
|---|
| Sodium Monofluorophosphate
Monofluorophosphate is a competitive inhibitor of pyruvate kinase and alkaline phosphatase with Ki of 3.4 mM and 69 μM, respectively, which also irreversibly inhibits phosphorylase phosphatase with Ki of 0.5 mM. |
| PKM2-IN-1
PKM2-IN-1 (compound 3k) is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM. The IC50 value for PKM1 is 4-5-fold higher than that for PKM2. |
| TEPP-46
Ml-265 (TEPP-46) is an effective activator of pyruvate kinase M2 (PKM2). |
| Mitapivat (AG-348)
Mitapivat (AG-348) is the first-in-class, oral effective pyruvate kinase small molecule allosteric activator. Mitapivat (AG-348) is active against wild-type and various mutated PKR enzymes, and promotes healthy red blood cell generation by activating mutated PKR to increase ATP levels. |
| Etavopivat
Etavopivat, an oral erythrocyte pyruvate kinase activator, is being developed for sickle cell disease and other hemoglobinopathies, previously reported in 2019. |
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