| Bioactivity | GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively[1]. | ||||||||||||
| Invitro | Hematopoietic progenitor kinase-1 (HPK1), a serine/threonine Ste20-related protein kinase whose expression is restricted to the hematopoietic compartment (e.g., T cells, B cells, and dendritic cells), is one such kinase. HPK1 is a negative-feedback regulator of T cell receptor signaling, which dampens T cell proliferation and effector function[1]. | ||||||||||||
| Name | GNE-1858 | ||||||||||||
| CAS | 2680616-96-8 | ||||||||||||
| Formula | C21H26F2N8 | ||||||||||||
| Molar Mass | 428.48 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Wu P, et al. Hematopoietic Progenitor Kinase-1 Structure in a Domain-Swapped Dimer. Structure. 2019 Jan 2;27(1):125-133.e4. |
GNE-1858
CAS: 2680616-96-8 F: C21H26F2N8 W: 428.48
GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 n
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