GNF-2

Biochem/physiol Actions

GNF-2 belongs to a new class of Bcr-abl inhibitors. GNF-2 appears to bind to the myristoyl binding pocket, an allosteric site distant from the active site, stabilizing the inactive form of the kinase. It inhibits Bcr-abl phosphorylation with an IC₅₀ of 267 nM, but does not inhibit a panel of 63 other kinases, including native c-Abl, and shows complete lack of toxicity towards cells not expressing Bcr-Abl. GNF-2 shows great potential for a new class of inhibitor to study Bcr-abl activity and to treat resistant Chronic myelogenous leukemia (CML), which is caused the Bcr-Abl oncoprotein.

Features and Benefits

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This compound is featured on the Abl page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Molecular Weight: 374.32. Empirical Formula: C₁₈H₁₃F₃N₄O₂. Quality Level: 100. Assay: ≥. 98% (HPLC). form: solid. color: off-white. solubility: H₂O: <. 2 . mg/mL, DMSO: ≥. 5 . mg/mL. storage temp.: 2-8°C. SMILES string: NC(: O)c1cccc(c1)-c2cc(Nc3ccc(OC(F)(F)F)cc3)ncn2. InChI: 1S/C18H13F3N4O2/c19-18(20,21)27-14-6-4-13(5-7-14)25-16-9-15(23-10-24-16)11-2-1-3-12(8-11)17(22)26/h1-10H,(H2,22,26)(H,23,24,25). InChI key: WEVYNIUIFUYDGI-UHFFFAOYSA-N. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Personal Protective Equipment: dust mask type N95 (US), Eyeshields, Gloves.