Tyrosine kinase is a large group of proteins regulates the function of cell growth, differentiation, motility, cytoskeletal rearrangement and adhesion etc. They activate the target protein through transfer of phosphate from ATP to the hydroxyl group of a target protein tyrosine. Transmembrane receptor kinases and non-receptor cytoplasmic kinases are two main categories of the tyrosine kinases.
Receptor tyrosine kinases bind to extracellular ligands/growth factors, which promotes receptor dimerization and autophosphorylation of receptor tyrosine residues. This triggers a cascade of downstream events through phosphorylation of intracellular proteins that ultimately transduce the extracellular signal to the nucleus, causing changes in gene expression. Receptor tyrosine kinases include EGFR/ErbB, PDGFR, VEGFR, FGFR and MET subfamilies etc. Dysfunctions in tyrosine phosphorylation are linked to oncogenic transformation. In additions, various adaptor and effector proteins couple to carboxy-terminal of an active kinase. For instance, binding of the GRB2 adaptor protein activates EGFR and MAPK/ERK signaling.
Non-receptor tyrosine kinases involve many well-defined proteins (e.g. the Src family kinases, c-Abl, and Jak kinases) and other kinases which regulates cell growth and differentiation. For example, Src family kinases are curial for activating and inhibitory pathways in the innate immune response.
Items 1-10 of 363
- EAI045Catalog No. :B6054Inhibitor of L858R/T790M EGFR mutants
- CTX0294885Catalog No. :B5843Pan-kinase inhibitorCTx-0294885 is a novel bisanilino pyrimidine. It has inhibitory activity towards a wild range of kinases in vitro.
- BLU9931Catalog No. :A8706FGFR4 inhibitor,potent and irreversibleBLU9931 is a potent and irreversible inhibitor of FGFR4.
- AG957Catalog No. :C5826a tyrphostin that targets transforming Bcr-Abl fusion proteins
- AG-1295Catalog No. :C5465potent and selective inhibitor of PDGF receptor kinase
- AG-1557Catalog No. :C5417inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase
- HA-100 (hydrochloride)Catalog No. :C4953inhibitor of protein kinases (PKs)
- AG-183Catalog No. :C4844inhibitor of epidermal growth factor (EGF) receptor kinase
- Tandutinib (MLN518) HClCatalog No. :B7853FLT3 inhibitor,potent and selective
- HNMPACatalog No. :C5553cell impermeable tyrosine kinase inhibitor