ON044580 is a potent non-ATP-competitive inhibitor of the JAK2 kinase, demonstrating IC50 values of 1.23 μM and 1.09 μM for wild-type and V617F mutant JAK2, respectively. This compound functions by either binding to the STAT-5 binding domain or an allosteric site of JAK2, leading to the suppression of JAK2 kinase activity. ON044580 effectively induces apoptosis in chronic myelogenous leukemia cells that exhibit resistance to Imatinib, and it also inhibits both wild-type and T315I mutant forms of the BCR-ABL kinase. This reagent holds promise for therapeutic applications in myeloproliferative disorders characterized by dysregulated JAK/STAT signaling.
ON044580 is a potent non-ATP-competitive inhibitor of the JAK2 kinase, demonstrating IC50 values of 1.23 μM and 1.09 μM for wild-type and V617F mutant JAK2, respectively. This compound functions by either binding to the STAT-5 binding domain or an allosteric site of JAK2, leading to the suppression of JAK2 kinase activity. ON044580 effectively induces apoptosis in chronic myelogenous leukemia cells that exhibit resistance to Imatinib, and it also inhibits both wild-type and T315I mutant forms of the BCR-ABL kinase. This reagent holds promise for therapeutic applications in myeloproliferative disorders characterized by dysregulated JAK/STAT signaling.
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