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kinase selectivity analysis

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Inhibitors & Agonists

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Fluorescent Dye

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-D2415

    Fluorescent Dye Others
    BODIPY-FL staurosporine (Compound 8a) is a fluorescence probe based on staurosporine, exhibiting high specificity towards tyrosine kinases (TK) and tyrosine kinase-like (TKL) family kinases. BODIPY-FL staurosporine has the potential to develop binding assays for kinases that are not recommended for use with Kinase Tracer 236, such as PIM3, CDC42BPG, MAP2K7, TXK, and SIK3. BODIPY-FL staurosporine can be a powerful tool for analyzing kinase selectivity in kinase drug discovery .
    BODIPY-FL staurosporine
  • HY-121708

    c-Kit Cancer
    KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.
    KI-328

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