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For research use only. Not Intended for Therapeutic Use!
Cat No:I008473
Synonyms:OPB31121; OPB-31121; OPB 31121;;NONE
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Appearance:Solid powder
Purity: > 98%
Cat No:I008473
OPB-31121 is an orally bioavailable inhibitor of signal transducer and activator of transcription 3 (STAT3), with potential antineoplastic activity. OPB-31121 inhibits the phosphorylation of STAT3, which prevents binding of STAT3 to DNA sequences on a variety of STAT3-responsive promoters and may result in the inhibition of STAT3-mediated transcription and, potentially, the inhibition of tumor cell proliferation. STAT3 is constitutively activated in a variety of cancers, contributing to the loss of cell growth control and neoplastic transformation.
Originator: Otsuka Pharmaceutical
Class: Antineoplastics
Mechanism of Action: STAT3 transcription factor inhibitors
Orphan Drug Status: No
New Molecular Entity: Yes

1:Hitting the right spot: Mechanism of action of OPB-31121, a novel and potent inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3). Brambilla L, Genini D, Laurini E, Merulla J, Perez L, Fermeglia M, Carbone GM, Pricl S, Catapano CV.Mol Oncol. 2015 Jun;9(6):1194-206. doi: 10.1016/j.molonc.2015.02.012. Epub 2015 Mar 5. PMID: 25777967 Free Article
2:Phase I Study of OPB-31121, an Oral STAT3 Inhibitor, in Patients with Advanced Solid Tumors. Oh DY, Lee SH, Han SW, Kim MJ, Kim TM, Kim TY, Heo DS, Yuasa M, Yanagihara Y, Bang YJ.Cancer Res Treat. 2015 Oct;47(4):607-15. doi: 10.4143/crt.2014.249. Epub 2015 Feb 26. PMID: 25715763 Free PMC Article
3:Phase 1 and pharmacological trial of OPB-31121, a signal transducer and activator of transcription-3 inhibitor, in patients with advanced hepatocellular carcinoma. Okusaka T, Ueno H, Ikeda M, Mitsunaga S, Ozaka M, Ishii H, Yokosuka O, Ooka Y, Yoshimoto R, Yanagihara Y, Okita K.Hepatol Res. 2015 Dec;45(13):1283-91. doi: 10.1111/hepr.12504. Epub 2015 Mar 24. PMID: 25676869
4:Phase 1, open-label, dose-escalation, and pharmacokinetic study of STAT3 inhibitor OPB-31121 in subjects with advanced solid tumors. Bendell JC, Hong DS, Burris HA 3rd, Naing A, Jones SF, Falchook G, Bricmont P, Elekes A, Rock EP, Kurzrock R.Cancer Chemother Pharmacol. 2014 Jul;74(1):125-30. doi: 10.1007/s00280-014-2480-2. Epub 2014 May 13. PMID: 24819685
5:A novel STAT inhibitor, OPB-31121, has a significant antitumor effect on leukemia with STAT-addictive oncokinases. Hayakawa F, Sugimoto K, Harada Y, Hashimoto N, Ohi N, Kurahashi S, Naoe T.Blood Cancer J. 2013 Nov 29;3:e166. doi: 10.1038/bcj.2013.63. PMID: 24292418 Free PMC Article
6:OPB-31121, a novel small molecular inhibitor, disrupts the JAK2/STAT3 pathway and exhibits an antitumor activity in gastric cancer cells. Kim MJ, Nam HJ, Kim HP, Han SW, Im SA, Kim TY, Oh DY, Bang YJ.Cancer Lett. 2013 Jul 10;335(1):145-52. doi: 10.1016/j.canlet.2013.02.010. Epub 2013 Feb 10. PMID: 23402820
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