AZ505

AZ505 is a **potent and selective small molecule inhibitor** of the lysine methyltransferase SET and MYND domain-containing protein 2 (SMYD2), which catalyzes the methylation of both histone and non-histone proteins, including tumor suppressor proteins such as p53 and Rb. AZ505 binds competitively with the substrate peptide in the SMYD2 peptide-binding groove and is highly selective for SMYD2 over other related methyltransferases (IC50 for SMYD2 inhibition: 0.12 μM)[4][7][10]. Preclinical research has shown that AZ505 can suppress proliferation of cancer cells, inhibit tumor growth, and affect bone metabolism by altering osteoblast and osteoclast differentiation. Despite its positive effects on bone formation in vitro, AZ505 demonstrated a catabolic effect on bone mass in vivo, attributed to increased RANKL expression and bone resorption[1][3]. It has also been shown to modulate inflammatory responses and has been studied in mouse models of breast cancer and polycystic kidney disease[1]. AZ505 is used primarily as a research compound and is not approved for human use.

Other names

AZ 505AZ505AZ-505AZ505 ditrifluoroacetateAZ-505 ditrifluoroacetateAZ 505 ditrifluoroacetate