HO-3867, an analog of curcumin, is a selective STAT3 inhibitor.

HO3867 produces significant cytotoxicity in A2780 and other tested ovarian cancer cell lines, with less toxic to noncancerous ovarian surface epithelial cells. HO-3867 induces G(2)-M cell cycle arrest in A2780 cells and promotes apoptosis by caspase-8 and caspase-3 activation. HO-3867 blocks the JAK/STAT3 pathway in human ovarian cancer cell lines. [1]

 HO-3867 (100 ppm p.o.) inhibits the growth of ovarian cancer xenograft tumor in mice without any apparent signs of toxicity, and also results in inhibition of pSTAT3 as well as downregulation of the STAT3-targeting proteins. [1] HO-3867 sensitizes cisplatin-resistant ovarian carcinoma through STAT3 inhibition. [2] HO-3867 (100 ppm p.o.) also attenuates left-heart-failure-induced pulmonary hypertension by decreasing oxidative stress and increasing PTEN expression in the lung of rats. [3]

 

References

[1] Selvendiran K, et al. Mol Cancer Ther. 2010, 9(5), 1169-1179.

[2] Selvendiran K, et al. Cancer Biol Ther. 2011, 12(9), 837-845.

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