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Tyrosine Kinase

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.

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  1. EAI045
    Catalog No. :
    B6054
    Inhibitor of L858R/T790M EGFR mutants
  2. CTX0294885
    Catalog No. :
    B5843
    Pan-kinase inhibitor
    CTx-0294885 is a novel bisanilino pyrimidine. It has inhibitory activity towards a wild range of kinases in vitro.
  3. BLU9931
    Catalog No. :
    A8706
    FGFR4 inhibitor,potent and irreversible
    BLU9931 is a potent and irreversible inhibitor of FGFR4.
  4. AG957
    Catalog No. :
    C5826
    a tyrphostin that targets transforming Bcr-Abl fusion proteins
  5. AG-1295
    Catalog No. :
    C5465
    potent and selective inhibitor of PDGF receptor kinase
  6. AG-1557
    Catalog No. :
    C5417
    inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase
  7. HA-100 (hydrochloride)
    Catalog No. :
    C4953
    inhibitor of protein kinases (PKs)
  8. AG-183
    Catalog No. :
    C4844
    inhibitor of epidermal growth factor (EGF) receptor kinase
  9. Tandutinib (MLN518) HCl
    Catalog No. :
    B7853
    FLT3 inhibitor,potent and selective
  10. HNMPA
    Catalog No. :
    C5553
    cell impermeable tyrosine kinase inhibitor

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