Go 6976 is a potent FLT3 inihibtor which is been shown to initiate cytotoxicity involving acute leukemia. Also known as a PKC inhibitor, which results into apoptosis and tumor destruction. Cancer therapeutic agent.
Potent protein kinase C (PKC) inhibitor (IC 50 = 7.9 nM). In vitro, discriminates between Ca 2+ -dependent and -independent isoforms of PKC; selectively inhibits PKC α and PKC β 1 (IC 50 values are 2.3 and 6.2 nM respectively) but does not inhibit the activity of PKC δ , - ε , or - ζ (IC 50 > 3 μ M). Also inhibits TrkA, TrkB, JAK2 and JAK3 tyrosine kinases (IC 50 values are 5, 30, 130 and 370 nM respectively).
Gö6976 is an ATP-competitive PKC inhibitor specific for Ca2+-dependent PKCα and PKCβ1 isozymes. It is also a potent inhibitor of PKD. Researchers have demonstrated that Gö6976 blocks JNK activation and inhibits PKCα-mediated, TPA-stimulated phosphorylation of CREB at Ser133. Gö6976 is also an effective inhibitor of the tyrosine kinases Jak2 and FLT3, as well as TrkA and TrkB.
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