c-Fos Inhibitor

T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.

c-Fos-IN-1 (Compound P16) is a c-Jun inhibitor, and decreases mRNA levels and protein levels of c-Fos. c-Fos-IN-1 also inhibits the phosphorylation activity of ERK and the transcriptional activity of AP-1. c-Fos-IN-1 shows anticancer activity by inhibiting ERK/c-Fos/Jun pathway. c-Fos-IN-1 inhibits the proliferation and migration of gastric cancer cells (IC₅₀: 2.31 μM for MGC-803 cell). c-Fos-IN-1 arrests cell cycle at G2/M phase and induces cancer cell apoptosis. c-Fos-IN-1 inhibits gastric cancer tumor growth.

Amorphigenin is a trothotenone compound. Amorphigenin inhibits osteoclast differentiation by suppressing the expression of c-Fos and NFATc1 in activated T cells. Amorphigenin degrades melanosome proteins by activating the AMPK-dependent autophagy pathway, but not in dependence of the mTOR pathway. Amorphigenin significantly protects bone mass and reduces bone erosion in a mouse model of inflammatory bone loss. Amorphigenin can be used to study inflammatory bone diseases, postmenopausal osteoporosis, and skin pigmentation disorders.