MAP4K4-IN-3 (Compound 17) 是一种有效的选择性 MAP4K4 抑制剂，在激酶实验中 IC50 为 14.9 nM，在细胞实验中 IC50 为 470 nM。具有抗糖尿病活性。
货号:ajcx34940
CAS:1811510-58-3
分子式:C15H12ClN5
分子量：297.74
溶解度:DMSO : 10 mg/mL (33.59 mM; ultrasonic and warming and heat to 60°C)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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[1].

MAP4K4, a serine/threonine protein kinase may be a viable target for antidiabetic agents[1].

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[2].

[1]. 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.
[2]. 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.