FH535 is a β-catenin pathway inhibitor. FH535 represses pancreatic cancer xenograft growth and angiogenesis. FH535 increases the radiosensitivity and reverses epithelial-to-mesenchymal transition of radioresistant esophageal cancer cell line KYSE-150R. FH535 inhibited metastasis and growth of pancreatic cancer cells. FH535 selectively inhibits cell proliferation and potentiates imatinib-induced apoptosis in myeloid leukemia cell lines.
1: Liu L, Zhi Q, Shen M, Gong FR, Zhou BP, Lian L, Shen B, Chen K, Duan W, Wu MY, Tao M, Li W. FH535, a β-catenin pathway inhibitor, represses pancreatic cancer xenograft growth and angiogenesis. Oncotarget. 2016 Jul 26;7(30):47145-47162. doi: 10.18632/oncotarget.9975. PubMed PMID: 27323403.
2: Su H, Jin X, Zhang X, Zhao L, Lin B, Li L, Fei Z, Shen L, Fang Y, Pan H, Xie C. FH535 increases the radiosensitivity and reverses epithelial-to-mesenchymal transition of radioresistant esophageal cancer cell line KYSE-150R. J Transl Med. 2015 Mar 31;13:104. doi: 10.1186/s12967-015-0464-6. PubMed PMID: 25888911; PubMed Central PMCID: PMC4384308.
3: Wu MY, Liang RR, Chen K, Shen M, Tian YL, Li DM, Duan WM, Gui Q, Gong FR, Lian L, Li W, Tao M. FH535 inhibited metastasis and growth of pancreatic cancer cells. Onco Targets Ther. 2015 Jul 6;8:1651-70. doi: 10.2147/OTT.S82718. PubMed PMID: 26185454; PubMed Central PMCID: PMC4500609.
4: Suknuntha K, Thita T, Togarrati PP, Ratanachamnong P, Wongtrakoongate P, Srihirun S, Slukvin I, Hongeng S. Wnt signaling inhibitor FH535 selectively inhibits cell proliferation and potentiates imatinib-induced apoptosis in myeloid leukemia cell lines. Int J Hematol. 2016 Oct 20. [Epub ahead of print] PubMed PMID: 27766528.
5: Tomizawa M, Shinozaki F, Motoyoshi Y, Sugiyama T, Yamamoto S, Ishige N. FH535 suppresses the proliferation and motility of hepatocellular carcinoma cells. Int J Oncol. 2016 Jan;48(1):110-4. doi: 10.3892/ijo.2015.3220. PubMed PMID: 26530115.
6: Gedaly R, Galuppo R, Daily MF, Shah M, Maynard E, Chen C, Zhang X, Esser KA, Cohen DA, Evers BM, Jiang J, Spear BT. Targeting the Wnt/β-catenin signaling pathway in liver cancer stem cells and hepatocellular carcinoma cell lines with FH535. PLoS One. 2014 Jun 18;9(6):e99272. doi: 10.1371/journal.pone.0099272. PubMed PMID: 24940873; PubMed Central PMCID: PMC4062395.
7: Liu J, Li G, Liu D, Liu J. FH535 inhibits the proliferation of HepG2 cells via downregulation of the Wnt/β-catenin signaling pathway. Mol Med Rep. 2014 Apr;9(4):1289-92. doi: 10.3892/mmr.2014.1928. PubMed PMID: 24482011.
8: Iida J, Dorchak J, Lehman JR, Clancy R, Luo C, Chen Y, Somiari S, Ellsworth RE, Hu H, Mural RJ, Shriver CD. FH535 inhibited migration and growth of breast cancer cells. PLoS One. 2012;7(9):e44418. doi: 10.1371/journal.pone.0044418. PubMed PMID: 22984505; PubMed Central PMCID: PMC3439405.
9: Polk WW. FH535 potentiation of cigarette smoke condensate cytotoxicity is associated with changes in β-catenin and EGR-1 signaling. Int J Toxicol. 2012 Jul-Aug;31(4):380-9. doi: 10.1177/1091581812447956. PubMed PMID: 22713211.
10: Kril LM, Vilchez V, Jiang J, Turcios L, Chen C, Sviripa VM, Zhang W, Liu C, Spear B, Watt DS, Gedaly R. N-Aryl benzenesulfonamide inhibitors of [3H]-thymidine incorporation and β-catenin signaling in human hepatocyte-derived Huh-7 carcinoma cells. Bioorg Med Chem Lett. 2015 Sep 15;25(18):3897-9. doi: 10.1016/j.bmcl.2015.07.040. PubMed PMID: 26243371; PubMed Central PMCID: PMC4540627.
11: Galuppo R, Maynard E, Shah M, Daily MF, Chen C, Spear BT, Gedaly R. Synergistic inhibition of HCC and liver cancer stem cell proliferation by targeting RAS/RAF/MAPK and WNT/β-catenin pathways. Anticancer Res. 2014 Apr;34(4):1709-13. PubMed PMID: 24692700.
12: Umazume K, Tsukahara R, Liu L, Fernandez de Castro JP, McDonald K, Kaplan HJ, Tamiya S. Role of retinal pigment epithelial cell β-catenin signaling in experimental proliferative vitreoretinopathy. Am J Pathol. 2014 May;184(5):1419-28. doi: 10.1016/j.ajpath.2014.01.022. PubMed PMID: 24656918.
13: Handeli S, Simon JA. A small-molecule inhibitor of Tcf/beta-catenin signaling down-regulates PPARgamma and PPARdelta activities. Mol Cancer Ther. 2008 Mar;7(3):521-9. doi: 10.1158/1535-7163.MCT-07-2063. PubMed PMID: 18347139.
14: Wu MY, Xie X, Xu ZK, Xie L, Chen Z, Shou LM, Gong FR, Xie YF, Li W, Tao M. PP2A inhibitors suppress migration and growth of PANC-1 pancreatic cancer cells through inhibition on the Wnt/β-catenin pathway by phosphorylation and degradation of β-catenin. Oncol Rep. 2014 Aug;32(2):513-22. doi: 10.3892/or.2014.3266. PubMed PMID: 24926961; PubMed Central PMCID: PMC4091883.
15: Wachter J, Neureiter D, Alinger B, Pichler M, Fuereder J, Oberdanner C, Di Fazio P, Ocker M, Berr F, Kiesslich T. Influence of five potential anticancer drugs on wnt pathway and cell survival in human biliary tract cancer cells. Int J Biol Sci. 2012;8(1):15-29. PubMed PMID: 22211101; PubMed Central PMCID: PMC3226029.
16: Iwata M, Aikawa T, Hakozaki T, Arai K, Ochi H, Haro H, Tagawa M, Asou Y, Hara Y. Enhancement of Runx2 expression is potentially linked to β-catenin accumulation in canine intervertebral disc degeneration. J Cell Physiol. 2015 Jan;230(1):180-90. doi: 10.1002/jcp.24697. PubMed PMID: 24916026.
17: Kim HJ, Kang GJ, Kim EJ, Park MK, Byun HJ, Nam S, Lee H, Lee CH. Novel effects of sphingosylphosphorylcholine on invasion of breast cancer: Involvement of matrix metalloproteinase-3 secretion leading to WNT activation. Biochim Biophys Acta. 2016 Sep;1862(9):1533-43. doi: 10.1016/j.bbadis.2016.05.010. PubMed PMID: 27216977.
18: Ren J, Wang R, Song H, Huang G, Chen L. Secreted frizzled related protein 1 modulates taxane resistance of human lung adenocarcinoma. Mol Med. 2014 Apr 8;20:164-78. doi: 10.2119/molmed.2013.00149. PubMed PMID: 24643460; PubMed Central PMCID: PMC4002848.
19: Zhang S, Da L, Yang X, Feng D, Yin R, Li M, Zhang Z, Jiang F, Xu L. Celecoxib potentially inhibits metastasis of lung cancer promoted by surgery in mice, via suppression of the PGE2-modulated β-catenin pathway. Toxicol Lett. 2014 Mar 3;225(2):201-7. doi: 10.1016/j.toxlet.2013.12.014. PubMed PMID: 24374173.
20: Frewer KA, Sanders AJ, Owen S, Frewer NC, Hargest R, Jiang WG. A role for WISP2 in colorectal cancer cell invasion and motility. Cancer Genomics Proteomics. 2013 Jul-Aug;10(4):187-96. PubMed PMID: 23893926.
Chemical |
CAS Num |
108409-83-2 |
Chemical Formula |
C13H10Cl2N2O4S |
Molecular Weight |
361.193 |
IUPAC Chemical Name |
2,5-dichloro-N-(2-methyl-4-nitrophenyl)-benzenesulfonamide |
Exact Mass |
359.9738 |
Elemental Analysis |
C, 43.23; H, 2.79; Cl, 19.63; N, 7.76; O, 17.72; S, 8.88 |
Synonym |
FH535; FH 535; FH-535. |
Solubility |
Soluble in DMSO |
SMILES Code |
O=S(C1=CC(Cl)=CC=C1Cl)(NC2=CC=C([N+]([O-])=O)C=C2C)=O |
Biological |
Targets and Effects |
N/A |
Pathways |
Apoptosis |
Physical |
Appearance |
Solid powder |
Purity |
>98% (or refer to the Certificate of Analysis) |
Shipping Condition |
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
Storage Condition |
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Shelf Life |
>2 years if stored properly |