MAP4K4-IN-3 (Compound 17) is a potent and selective MAP4K4 inhibitor with an IC₅₀ of 14.9 nM in kinase assay, an IC₅₀ of 470 nM in cell assay. Antidiabetic agent.

MAP4K4, a serine/threonine protein kinase may be a viable target for antidiabetic agents.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Oral dosing in telemetered rats for 5 days with MAP4K4-IN-3 (Compound 2; 25 mg/kg, b.i.d.) results in a number of adverse effects. Substantial weight losses (7%) and body temperature increases (0.4°C) relative to controls are observed over the course of the study. For cardiovascular end points, maximal heart rate increases of 25 bpm, relative to controls, are induced by treatment with MAP4K4-IN-3.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Oral dosing in telemetered rats for 5 days with MAP4K4-IN-3 (Compound 2; 25 mg/kg, b.i.d.) results in a number of adverse effects. Substantial weight losses (7%) and body temperature increases (0.4°C) relative to controls are observed over the course of the study. For cardiovascular end points, maximal heart rate increases of 25 bpm, relative to controls, are induced by treatment with MAP4K4-IN-3.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Ammirati M, et al. Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based AntidiabeticTreatment. ACS Med Chem Lett. 2015 Oct 6;6(11):1128-33.  [Content Brief]

  . Dow RL, et al. 2-Aminopyridine-Based Mitogen-Activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4) Inhibitors: Assessment of Mechanism-Based Safety. J Med Chem. 2018 Apr 12;61(7):3114-3125.  [Content Brief]