RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pKi=9.04). It strongly suppresses necroptotic cell death and phosphorylation of MLKL (pMLKL) in human colorectal adenocarcinoma HT-29 cells (necroptosis, IC50=2 nM; pMLKL, IC50=1.3 nM) as well as mouse L-cells NCTC 929 (necroptosis, IC50=15 nM; pMLKL, IC50=2.7 nM).
- Highly potent RIP1 kinase inhibitor
- Orally available
- Brain-penetrating
- Suppresses necroptotic cell death
- Suppresses phosphorylation of MLKL (pMLML)