Биологическая активность
HPK1 ингибитор 1 is a highly мощный, селективный ингибитор of HPK1/MAP4K1 with biochemical IC50 of 0.0465 nM; displays >100-fold selectivity against 260 kinases in a panel of 265 kinases; HPK1 ингибитор 1 decreased SLP-76 phosphorylation in a human pSLP-76 ELISA at an IC50 lower than 0.02 uM; HPK1 ингибитор 1 enhanced Th1 cytokine production in T cells and fully reverted immune suppression imposed by the prostaglandin E2 (PGE2) and adenosine pathways in human T cells; HPK1 ингибитор 1 demonstrated a synergistic effect, resulting in enhanced interferon (IFN)-γ production when combination with pembrolizumab in human PBMCs
Оригинал на английском
HPK1 inhibitor 1 is a highly potent, selective inhibitor of HPK1/MAP4K1 with biochemical IC50 of 0.0465 nM; displays >100-fold selectivity against 260 kinases in a panel of 265 kinases; HPK1 inhibitor 1 decreased SLP-76 phosphorylation in a human pSLP-76 ELISA at an IC50 lower than 0.02 uM; HPK1 inhibitor 1 enhanced Th1 cytokine production in T cells and fully reverted immune suppression imposed by the prostaglandin E2 (PGE2) and adenosine pathways in human T cells; HPK1 inhibitor 1 demonstrated a synergistic effect, resulting in enhanced interferon (IFN)-γ production when combination with pembrolizumab in human PBMCs
Химические свойства
- CAS №
- 2246358-08-5
- Брутто-формула
- C₂₅H₂₇FN₈O
- Мол. масса
- 474.54 г/моль
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.