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Chemical Structure : AG-946
Catalog No.: PC-21605Not For Human Use, Lab Use Only.
AG-946 (AG946) is a potent, allosteric activator of wild-type and mutant RBC-specific form of pyruvate kinase (PKR) with AC50 of 5 nM for human wild-type PK, 4.3 nM and 6.9 nM for mutated K410E and R510Q PK proteins, resepctively.
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AG-946 (AG946) is a potent, allosteric activator of wild-type and mutant RBC-specific form of pyruvate kinase (PKR) with AC50 of 5 nM for human wild-type PK, 4.3 nM and 6.9 nM for mutated K410E and R510Q PK proteins, resepctively.
AG-946 activates both WT PKR and a panel of prototypically unstable PKR mutants.
AG-946 stabilizes PKR R510Q, an unstable mutant PKR enzyme, and preserves its catalytic activity under increasingly denaturing conditions.
AG-946 demonstrated good activity in cell-based assays using purified RBCs, with an average AC50 for PKR activation of 35 nM and an average maximum percent PKR activation of 197%.
AG-946 represents a new investigational PK activator with potential for low projected human drug load and long pharmacodynamic duration of action, suitable for clinical development in a broad range of hemolytic anemias and diseases characterized by dyserythropoiesis.
| M.Wt | 392.44 | |
| Formula | C18H16N8OS | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Liu T, et al. ChemMedChem. 2023 Dec 18:e202300559.
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