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GNE-1858 is a potent, and ATP-competitive inhibitor of hematopoietic progenitor kinase-1 (HPK1). GNE-1858 against wild-type and active mimetic mutants HPK1-TSEE and HPK1-SA with IC50 values of 1.9 nM, 1.9 nM and 4.5 nM, respectively. Hematopoietic progenitor kinase-1 (HPK1) is a negative-feedback regulator of T cell receptor signaling, which dampens T cell proliferation and effector function.
| Molecular Weight | 428.48 |
| Formula | C21H26F2N8 |
| CAS Number | 2680616-96-8 |
| Solubility (25°C) | DMSO ≥ 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Ping Wu, et al. Structure. Hematopoietic Progenitor Kinase-1 Structure in a Domain-Swapped Dimer
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