Drug intelligence / Profile preview

PF-06260933 dihydrochloride

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

PF-06260933 dihydrochloride is a potent and selective small molecule inhibitor of Mitogen-Activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4, also known as HGK), originally developed by Pfizer. It also exhibits inhibitory activity against related kinases MINK and TNIK. As an orally active research tool, it has been utilized to investigate the role of MAP4K4 in various pathological conditions, including fasting hyperglycemia in diabetic mouse models, vascular inflammation, and atherosclerosis. Recent research has also explored its potential in oncology, specifically in inhibiting tumor cell invasion in pediatric glioblastoma and lung adenocarcinoma, as well as its neuroprotective effects in motor neurons. It is currently used exclusively for research purposes and is not approved for therapeutic use in humans.

Other names
5-(4-Chlorophenyl)-[3,3'-bipyridine]-6,6'-diamine dihydrochloride
02

Targets

MAP4K4 (Mitogen-activated protein kinase kinase kinase kinase 4)KCNE1 (Misshapen-like kinase 1)TNIK (TRAF2- and NCK-interacting kinase)

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