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HO-3867 is a novel curcumin analog and a selective inhibitor of STAT3. [1]

STAT3 (signal transducer and activator of transcription 3) belongs to the STAT protein family. It mediates various gene expressions for numerous cellular functions, including cell growth, division and apoptosis.

HO-3867 selectively blocked STAT3 phosphorylation, transcription, and DNA binding without inhibiting other STATs proteins. It activated apoptosis in ovarian cancer cells and showed minimal toxicity to healthy cells. [2] HO-3867 also significantly inhibited the proliferation of serum-stimulated SMCs and elevated the phosphorylated and total levels of PTENs in SMCs. [3] By inducing cell cycle arrest and apoptosis, HO-3867 reduced the high levels of pSTAT3 Ser727 in endometrial cancer cells. [4]

In mice tumor xenograft, HO-3867 inhibited the tumor growth without toxic side effects, it also blocked PSTAT3/JAK1 and increased apoptotic marker cleaved Caspase 3/PARP. [2] [5] After rat carotid artery injury, HO-3867 inhibited neointima formation and upregulated PTEN expression. [3]

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