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Drug intelligence / Profile preview
PF-4618433
- Development stage
- Discontinued
- Lead developer
- Pfizer
- Modality
- Small Molecules
01
Overview
PF-4618433 is a potent, selective, small-molecule inhibitor of proline-rich tyrosine kinase 2 (PYK2, also known as PTK2B) with an IC50 of 637 nM. Developed by Pfizer, PF-4618433 binds to PYK2 in a unique inactive 'DFG-out' conformation, which provides superior selectivity for PYK2 over the closely related focal adhesion kinase (FAK) and other kinases such as p38. In preclinical research, PF-4618433 has been shown to promote osteogenesis, enhance osteoblast proliferation and differentiation, and increase mineralization in human mesenchymal stem cell (hMSC) cultures. It is primarily utilized as a chemical probe and research reagent to investigate the role of PYK2 in bone remodeling, osteoporosis, and other signaling pathways.
- Other names
- 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[5-(pyridin-3-yloxymethyl)-1H-pyrazol-3-yl]ureaPF 4618433PF4618433PF-4618433
02
Targets
PTK2B
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