Product Overview
GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 100 to 300 nM in various cell lines. BCR-ABL gene is fused by the BCR and ABL1 genes. BCR-ABL increased production of tyrosine kinase and played an essential role in the pathogenesis of chronic myelogenous leukemia (CML). Unlike imatinib that competitively inhibited the ATP-binding site of BCR-ABL kinase activity, GNF-2 allosterically inhibited (through binding the myristate-binding site of ABL) the proliferation of BCR-ABL positive cell and induces cell apoptosis. In Ba/F3.p210 Bcr-abl-expressing cells, 48 h treatment of GNF-2 was able to inhibit the proliferation of cells with an IC50 value of 138 nM. In addition, GNF-2 has been found to inhibit E255V and Y253H mutant Ba/F3 cells cell growth, with an IC50 value of 268 and 194 nM, respectively. GNF-2 also caused growth inhibition of K562 and SUP-B15 with an IC50 value of 273 nM and 268 nM, respectively. Injecting with BCR-ABL-expressing Ba/F3-p210 cells, 4 % lymphocytes reduction in eperipheral blood was induced.
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