For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I045951 |
| CAS Number | 2680616-96-8 |
| Synonyms | N-[2-(3,3-difluoropyrrolidin-1-yl)-6-pyrrolidin-3-ylpyrimidin-4-yl]-1-propan-2-ylpyrazolo[4,3-c]pyridin-6-amine |
| Molecular Formula | C21H26F2N8 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H26F2N8/c1-13(2)31-17-8-18(25-10-15(17)11-26-31)28-19-7-16(14-3-5-24-9-14)27-20(29-19)30-6-4-21(22,23)12-30/h7-8,10-11,13-14,24H,3-6,9,12H2,1-2H3,(H,25,27,28,29) |
| InChIKey | JKPAJCPZQIJPPS-UHFFFAOYSA-N |
| SMILES | CC(C)N1C2=CC(=NC=C2C=N1)NC3=NC(=NC(=C3)C4CCNC4)N5CCC(C5)(F)F |
| 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. |
