HO-3867

• CAT Number: I000609
• CAS Number: 1172133-28-6
• Molecular Formula: C28H30F2N2O2
• Molecular Weight: 464.6
• Purity: ≥95%
• Target: STAT
• Solubility: DMSO ≥ 32 mg/mL
• Storage: Store at -20°C
• InChIKey: PWZQFTQMMAIRRM-JFMUQQRKSA-N

HO-3867 (CAT: I000609) is a selective and potent inhibitor of STAT3 phosphorylation, transcription, and DNA binding. It specifically targets the STAT3 signaling pathway without affecting the expression of other active STAT proteins. In vitro, studies have shown that HO-3867 exhibits minimal toxicity towards noncancerous cells and tissues while inducing apoptosis in ovarian cancer cells. It inhibits cell migration, invasion, and survival by suppressing STAT3 phosphorylation. Additionally, HO-3867 has demonstrated efficacy in BRCA-mutated ovarian cancer cells, promoting apoptosis and increasing the levels of cleaved caspase-3, caspase-7, and PARP. Furthermore, HO-3867 in combination with cisplatin has shown significant inhibition of cell proliferation in cisplatin-resistant cells. These findings highlight the potential of HO-3867 as a therapeutic agent for targeting STAT3 signaling in ovarian cancer treatment.

Reference

1:A novel STAT3 inhibitor HO-3867 induces cell apoptosis by reactive oxygen species-dependent endoplasmic reticulum stress in human pancreatic cancer cells. Hu Y, Zhao C, Zheng H, Lu K, Shi D, Liu Z, Dai X, Zhang Y, Zhang X, Hu W, Liang G.Anticancer Drugs. 2017 Apr;28(4):392-400. doi: 10.1097/CAD.0000000000000470. PMID: 28067673 2:Aberrantly activated pSTAT3-Ser727 in human endometrial cancer is suppressed by HO-3867, a novel STAT3 inhibitor. Tierney BJ, McCann GA, Naidu S, Rath KS, Saini U, Wanner R, Kuppusamy P, Suarez A, Goodfellow PJ, Cohn DE, Selvendiran K.Gynecol Oncol. 2014 Oct;135(1):133-41. doi: 10.1016/j.ygyno.2014.07.087. Epub 2014 Jul 16. PMID: 25038288 Free PMC Article3:HO-3867, a safe STAT3 inhibitor, is selectively cytotoxic to ovarian cancer. Rath KS, Naidu SK, Lata P, Bid HK, Rivera BK, McCann GA, Tierney BJ, Elnaggar AC, Bravo V, Leone G, Houghton P, Hideg K, Kuppusamy P, Cohn DE, Selvendiran K.Cancer Res. 2014 Apr 15;74(8):2316-27. doi: 10.1158/0008-5472.CAN-13-2433. Epub 2014 Mar 3. PMID: 24590057 Free PMC Article4:HO-3867, a STAT3 inhibitor induces apoptosis by inactivation of STAT3 activity in BRCA1-mutated ovarian cancer cells. Tierney BJ, McCann GA, Cohn DE, Eisenhauer E, Sudhakar M, Kuppusamy P, Hideg K, Selvendiran K.Cancer Biol Ther. 2012 Jul;13(9):766-75. doi: 10.4161/cbt.20559. PMID: 22801507 5:HO-3867, a curcumin analog, sensitizes cisplatin-resistant ovarian carcinoma, leading to therapeutic synergy through STAT3 inhibition. Selvendiran K, Ahmed S, Dayton A, Kuppusamy ML, Rivera BK, Kálai T, Hideg K, Kuppusamy P.Cancer Biol Ther. 2011 Nov 1;12(9):837-45. doi: 10.4161/cbt.12.9.17713. Epub 2011 Nov 1. PMID: 21885917 6:Amelioration of doxorubicin-induced cardiotoxicity by an anticancer-antioxidant dual-function compound, HO-3867. Dayton A, Selvendiran K, Meduru S, Khan M, Kuppusamy ML, Naidu S, Kálai T, Hideg K, Kuppusamy P.J Pharmacol Exp Ther. 2011 Nov;339(2):350-7. doi: 10.1124/jpet.111.183681. Epub 2011 Jul 28. PMID: 21799049 Free PMC Article7:Cellular uptake, retention and bioabsorption of HO-3867, a fluorinated curcumin analog with potential antitumor properties. Dayton A, Selvendiran K, Kuppusamy ML, Rivera BK, Meduru S, Kálai T, Hideg K, Kuppusamy P.Cancer Biol Ther. 2010 Nov 15;10(10):1027-32. doi: 10.4161/cbt.10.10.13250. Epub 2010 Nov 15. PMID: 20798598 Free PMC Article8:HO-3867, a synthetic compound, inhibits the migration and invasion of ovarian carcinoma cells through downregulation of fatty acid synthase and focal adhesion kinase. Selvendiran K, Ahmed S, Dayton A, Ravi Y, Kuppusamy ML, Bratasz A, Rivera BK, Kálai T, Hideg K, Kuppusamy P.Mol Cancer Res. 2010 Sep;8(9):1188-97. doi: 10.1158/1541-7786.MCR-10-0201. Epub 2010 Aug 16. PMID: 20713491 Free PMC Article9:Anticancer efficacy of a difluorodiarylidenyl piperidone (HO-3867) in human ovarian cancer cells and tumor xenografts. Selvendiran K, Tong L, Bratasz A, Kuppusamy ML, Ahmed S, Ravi Y, Trigg NJ, Rivera BK, Kálai T, Hideg K, Kuppusamy P.Mol Cancer Ther. 2010 May;9(5):1169-79. doi: 10.1158/1535-7163.MCT-09-1207. Epub 2010 May 4. PMID: 20442315 Free PMC Article10:Inhibition of vascular smooth-muscle cell proliferation and arterial restenosis by HO-3867, a novel synthetic curcuminoid, through up-regulation of PTEN expression. Selvendiran K, Kuppusamy ML, Bratasz A, Tong L, Rivera BK, Rink C, Sen CK, Kálai T, Hideg K, Kuppusamy P.J Pharmacol Exp Ther. 2009 Jun;329(3):959-66. doi: 10.1124/jpet.108.150367. Epub 2009 Mar 10. PMID: 19276401 Free Article