RCGD 423 is a modulator of gp130.1 It increases levels of phosphorylated STAT3 and Myc in isolated pig articular chondrocytes (EC50s = 4.5-7.2 ?M), effects that can be reversed by the gp130 inhibitor SC144 . RCGD 423 reduces cellular apoptosis and hypertrophy induced by bone morphogenic protein 4 (BMP4) in isolated mouse total limb cells and isolated human healthy and osteoarthritic articular chondrocytes. In vivo, RCGD 423 (4 ?g/joint) reduces cartilage loss in a rat model of osteochondral injury.
1.Shkhyan, R., Van Handel, B., Bogdanov, J., et al.Drug-induced modulation of gp130 signalling prevents articular cartilage degeneration and promotes repairAnn. Rheum. Dis.77(5)760-769(2018)