Halofuginone lactate is a Febrifugine derivative that functions as a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. It specifically inhibits type-I collagen synthesis and can attenuate osteoarthritis by inhibiting TGF-β activity. Additionally, it acts as a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated, and store-operated Ca2+ channels. Halofuginone lactate has demonstrated anti-malaria, anti-inflammatory, anti-cancer, and anti-fibrosis effects.
- Competitively inhibits prolyl-tRNA synthetase.
- Specifically inhibits type-i collagen synthesis.
- Attenuates osteoarthritis through inhibition of TGF-β activity.
- Acts as a potent pulmonary vasodilator.
- Activates Kv channels and blocks various Ca2+ channels.
- Exhibits anti-malaria, anti-inflammatory, anti-cancer, and anti-fibrosis effects.