bwa4c

BWA4C is a small molecule inhibitor of 5-lipoxygenase (5-LO), an enzyme key for leukotriene biosynthesis in inflammatory pathways. Developed originally by GSK, BWA4C is a hydroxamic acid derivative that acts as an iron-ligand inhibitor, chelating the central iron atom in 5-LO and stabilizing its ferrous state, thereby suppressing the formation of pro-inflammatory leukotrienes from arachidonic acid[1][5][6]. BWA4C has demonstrated potent anti-proliferative and cytotoxic effects in various tumor cell lines, reducing viability independent of leukotriene suppression[2][7]. Additionally, it impairs osteoclastic bone resorption by reducing the recruitment and differentiation of osteoclast progenitors[3]. Newer findings suggest it also inhibits prostaglandin E2 export via the ATP-binding cassette transporter multidrug resistance protein 4 (MRP-4), contributing to its anti-inflammatory profile[4][5][6]. Despite these effects, clinical development was discontinued due to pharmacokinetic challenges and side effects, and it did not proceed to market approval[1][5].

Other names

N-(3-phenoxycinnamyl)acetohydroxamic acid