Aclacinomycin A HCl (75443-99-1) is a specific inhibitor of the 20S proteasome chymotrypsin-like activity.1 Inhibition of Brg1 proteasomal degradation by aclacinomycin A reverses (0.25 μM in ILU-18 cells ) the removal of Brg1 from promoters of inflammatory genes elucidating the regulatory role of the proteasome in controlling the duration of the inflammatory process.2 Induces the differentiation of K562 cells towards the erythroid pathway.3 Induces apoptosis.4 Cell permeable.
1) Figueiroda-Pereira et al. (1996), The Antitumor Drug Aclacinomycin A, Which Inhibits the Degradation of Ubiquitinated Proteins, Shows Selectivity for the Chymotrypsin-like Activity of the Bovine Pituitary 20S Proteasome; J. Biol. Chem., 271 16455
2) Cullen et al (2009), Catalytic activity of the proteasome fine-tunes Brg1-mediated chromatin remodeling to regulate the expression of inflammatory genes; Mol. Immunol., 47 600
3) Morceau et al. (2006), Tumor necrosis factor alpha inhibits aclacinomycin A-induced erythroid differentiation of K562 cells via GATA-1; Cancer Lett.. 240 203
4) Mayer et al. (1994), Culture conditions modulate the effects of alacinomycin A on growth, differentiation and apoptosis of HL60 cells; Anticancer Res., 14 2331