GNF-2

GNF-2 is an allosteric inhibitor of Bcr-Abl (IC₅₀ = 267 nM).¹ It is selective for Bcr-Abl over c-Abl and a panel of 63 additional kinases at 10 µM. It inhibits proliferation of Ba/F3 cells (IC₅₀ = 138 nM). GNF-2 (10 µM) reduces viral titers in Vero cells infected with infectious bronchitis virus (IBV), a coronavirus, via inhibition of IBV surface glycoprotein-induced syncytia formation and virus-cell fusion.² It inhibits LPS-induced production of nitric oxide (NO) and TNF-α in BV-2 microglia when used at concentrations of 10 and 20 µM.³ GNF-2 (1 and 10 mg/kg) reduces paw edema and increases the latency to paw withdrawal in a mouse model of inflammatory pain induced by complete Freund’s adjuvant (CFA). It also decreases mechanical and thermal hyperalgesia in a mouse model of diabetic neuropathy induced by streptozotocin (STZ; Item No. 13104).

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1. Adrián, F.J., Ding, Q., Sim, T., et al. Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat. Chem. Biol. 2(2), 95-102 (2006).

2. Sisk, J.M., Frieman, M.B., and Machamer, C.E. Coronavirus S protein-induced fusion is blocked prior to hemifusion by Able kinase inhibitors. J. Gen. Virol. 99(5), 619-630 (2018).

3. Song, G.J., Rahman, M.H., Jha, M.K., et al. A Bcr-Abl inhibitor GNF-2 attenuates inflammatory activation of glia and chronic pain. Front. Pharmacol. 10, 543 (2019).