Back to products

Browse products

Approved anticancer agents

Anticancer agents in trials

Anticancer molecular libraries

MedKoo product information:

S31-201 is benezoic acid based small molecule, which inhibits the Stat3 transcription factor by blocking the phosphorylation and dimerization events necessary for activation. Many cancers express aberrant behavior in the Stat3 growth factor, making this compound a valuable tool for perturbing the chemistry of such systems.

In HCC cells with loss of response to TGF-.beta., NSC 74859, a STAT3-specific inhibitor, markedly suppresses growth. In contrast, CD133+ status did not affect the response to STAT3 inhibition: both CD133+ Huh-7 cells and CD133- Huh-7 cells are equally sensitive to NSC 74859 treatment and STAT3 inhibition, with an IC50 of 100 .mu.M. Thus, the TGF-.beta./beta2 spectrin (.beta.2SP) pathway may reflect a more functional 'stem/progenitor' state than CD133. Furthermore, NSC 74859 treatment of Huh-7 xenografts in nude mice significantly retarded tumor growth, with an ED of only 5 mg/kg. Moreover, NSC 74859 inhibited tyrosine phosphorylation of STAT3 in HCC cells in vivo. The authors conclude that inhibiting interleukin 6 (IL6)/STAT3 in HCCs with inactivation of the TGF-.beta./.beta.2SP pathway is an effective approach in management of HCCs. Thus, IL6/STAT3, a major signaling pathway in HCC stem cell renewal and proliferation, can provide a novel approach to the treatment of specific HCCs.  see: Oncogene (2009), 28(7), 961-972.

Current developer:  H. Lee Moffitt Cancer Center & Research Institute, USA; University of South Florida; University of Central Florida

1. Pang M, Ma L, Gong R, Tolbert E, Mao H, Ponnusamy M, Chin YE, Yan H, Dworkin LD, Zhuang S. A novel STAT3 inhibitor, S3I-201, attenuates renal interstitial fibroblast activation and interstitial fibrosis in obstructive nephropathy. Kidney Int. 2010 Aug;78(3):257-68. Epub 2010 Jun 2. PubMed PMID: 20520592.

2. The STAT3 inhibitor NSC 74859 is effective in hepatocellular cancers with disrupted TGF-.beta. signaling. Lin, L.; Amin, R.; Gallicano, G. I.; Glasgow, E.; Jogunoori, W.; Jessup, J. M.; Zasloff, M.; Marshall, J. L.; Shetty, K.; Johnson, L.; Mishra, L.; He, A. R. Cancer Genetics, Digestive Diseases, and Developmental Molecular Biology, Department of Surgery, Georgetown University, Washington, DC, USA. Oncogene (2009), 28(7), 961-972.

3. Small molecule inhibitors of STAT3 with anti-tumor activity. Turkson, James; Sebti, Said M.; Guida, Wayne; Yip, Man Lun; Lawrence, Nicholas; Lawrence, Harshani; Greedy, Benjamin. (H. Lee Moffitt Cancer Center & Research Institute, USA; University of South Florida; University of Central Florida). PCT Int. Appl. (2007), 133pp. CODEN: PIXXD2 WO 2007136858 A2 20071129 Designated States W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SV, SY, TJ, TM, TN, TR, TT, TZ, UA. Designated States RW: AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IS, IT, LU, MC, MT, NL, PT, SE, TR, BF, BJ, CF, CG, CI, CM, GA, ML, MR, NE, SN, TD, TG. Patent written in English. Application: WO 2007-US12187 20070521. Priority: US 2006-801750 20060519.