RIPK1-IN-7 is a potent and selective RIPK1 inhibitor with a Kd of 4 nM and an enzymatic IC50 of 11 nM. RIPK1-IN-7 exhibits excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model[1]. IC50: 11 nM (RIPK1)[1]Kd: 4 nM (RIPK1)[1]
RIPK1-IN-7 shows potent cell protection effect in the TSZ-induced HT29 cell necroptosis model with an EC50 of 2nM[1].RIPK1-IN-7 displays considerable activity against several other kinases, such as Flt4, TrkA, TrkB, TrkC, Axl, HRI, Mer, and MAP4K5 with IC50s of 20, 26, 8, 7, 35, 26, 29, and 27 nM, respectively[1].
[1]. Li Y, et al. Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model. J Med Chem. 2018 Dec 27;61(24):11398-11414.