GNF-2
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CAS No. | 778270-11-4 | Cat. No. | BCP06315 |
Name | GNF-2 | ||
Synonyms | GNF2;GNF 2; | ||
SMILES | |||
Chemical Name | |||
Formula | C18H13F3N4O2 | M. Wt | 374.32 |
Purity | 98% | Storage | Store at 4-8°C |
Description | GNF-2 causes a dose-dependent growth inhibition of the Bcr-abl–positive cell lines with IC50 values of 273 nM (K562) and 268 nM (SUP-B15). GNF-2 inhibits the growth of Ba/F3.p210E255V and Ba/F3.p185Y253H cells with IC50 values of 268 nM and 194 nM respectively. GNF-2 (1 μM) induces apoptosis of Ba/F3.p210 cells as well as Ba/F3.p210E255V cells. GNF-2 inhibits the cellular tyrosine phosphorylation of Bcr-abl in a dose-dependent manner with IC50 of 267 nM. GNF-2 (1 μM) induces a significant decrease in the levels of phospho-Stat5 in Ba/F3.p210 cells. GNF-2 binds to the myristic binding pocket of Bcr-abl.GNF-2 inhibits the kinase activity of non-myristoylated c-Abl more potently than that of myristoylated c-Abl by binding to the myristate-binding pocket in the C-lobe of the kinase domain. GNF-2 (10 μM) requires BCR and/or the c-Abl SH3 and/or SH2 domains to inhibit BCR-Abl-dependent cell proliferation. GNF-2, but not a methylated GNF-2 analog, binds c-Abl in cellular extracts derived from |
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