Uses
4-[2-(2-Furanyl)-6-(4-nitrophenyl)-4-pyridinyl]benzamide is a inhibits MYC-induced oncogenic transformation in cell culture and blocks the growth of a xenotransplant of MYC-amplified human cancer cells.
Biological Activity
mkj pyr 9 is a novel small molecule inhibitor of myc, with the kd value of 6.5 ± 1.0 nm. besides, kj pyr 9 also suppresses the formation of myc-max and oncogenic transformation induced by myc in cell culture [1].
in vitro
in chicken embryo fibroblasts, kj pyr 9 was found to have the ability to interfere with the oncogenic activity of myc, with the best aqueous solubility. besides, in human b-cell line p493-6, 20 μm kj pyr 9 could significantly inhibit cell proliferation, and kj pyr 9 could also inhibit the proliferation of nci-h460, mda-mb-231, and sum-159pt cell lines, with the ic50 values between 5-10 μm. furthermore, treatment of p493-6 cells with kj pyr 9 could significantly suppress the transcription ability of myc [1].
in vivo
kj pyr 9 was found to have no acute toxicity in mouse and rat at a dose of 10 mg/kg, with an impressive ability to cross the blood-brain barrier. besides, in a mda-mb-231 cells xenograft tumor nude mice model, intraperitoneal injection with 10 mg/kg kj pyr 9 for 31 days could significantly inhibit tumor growth, while having no effect on the body weight [1].
References
[1] hart j r, garner a l, yu j, et al. inhibitor of myc identified in a kr?hnke pyridine library[j]. proceedings of the national academy of sciences, 2014, 111(34): 12556-12561.
