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FH535

FH535

  • CAT Number: I000367
  • CAS Number: 108409-83-2
  • Molecular Formula: C₁₃H₁₀Cl₂N₂O₄S
  • Molecular Weight: 361.2
  • Purity: ≥95%
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FH535(CAT: I000367) is a small molecule inhibitor that targets the Wnt/β-catenin signaling pathway. It was first identified as a compound that selectively induces apoptosis in cancer cells expressing wild-type p53 but not in cells with mutant p53. Further studies revealed that FH535 can inhibit the interaction between β-catenin and Tcf/Lef, which results in the downregulation of β-catenin target genes. FH535 has been shown to have anticancer effects in various types of cancer cells, including colon cancer, breast cancer, and hepatocellular carcinoma. In addition to its anticancer effects, FH535 has also been investigated for its potential in regenerative medicine, as it has been shown to promote cardiomyocyte differentiation and enhance neuronal differentiation of embryonic stem cells.

Catalog Number I000367
CAS Number 108409-83-2
Molecular Formula

C₁₃H₁₀Cl₂N₂O₄S

Purity 95%
Target Wnt/β-catenin
Solubility DMSO: ＞ 10 mM
Storage Store at -20°C
IC50 1.1 uM (Cytotoxicity in the CCLP-1 cell line) [1]
InChI InChI=1S/C13H10Cl2N2O4S/c1-8-6-10(17(18)19)3-5-12(8)16-22(20,21)13-7-9(14)2-4-11(13)15/h2-7,16H,1H3
InChIKey AXNUEXXEQGQWPA-UHFFFAOYSA-N
SMILES CC1=C(C=CC(=C1)[N+](=O)[O-])NS(=O)(=O)C2=C(C=CC(=C2)Cl)Cl
Reference

</br>1:Sorafenib and FH535 in combination act synergistically on hepatocellular carcinoma by targeting cell bioenergetics and mitochondrial function. Turcios L, Vilchez V, Acosta LF, Poyil P, Butterfield DA, Mitov M, Marti F, Gedaly R.Dig Liver Dis. 2017 Jan 19. pii: S1590-8658(17)30150-0. doi: 10.1016/j.dld.2017.01.146. [Epub ahead of print] PMID: 28179093 </br>2:Wnt signaling inhibitor FH535 selectively inhibits cell proliferation and potentiates imatinib-induced apoptosis in myeloid leukemia cell lines. Suknuntha K, Thita T, Togarrati PP, Ratanachamnong P, Wongtrakoongate P, Srihirun S, Slukvin I, Hongeng S.Int J Hematol. 2017 Feb;105(2):196-205. doi: 10.1007/s12185-016-2116-x. Epub 2016 Oct 20. PMID: 27766528 </br>3:FH535, a β-catenin pathway inhibitor, represses pancreatic cancer xenograft growth and angiogenesis. Liu L, Zhi Q, Shen M, Gong FR, Zhou BP, Lian L, Shen B, Chen K, Duan W, Wu MY, Tao M, Li W.Oncotarget. 2016 Jul 26;7(30):47145-47162. doi: 10.18632/oncotarget.9975. PMID: 27323403 Free PMC Article</br>4:FH535 suppresses the proliferation and motility of hepatocellular carcinoma cells. Tomizawa M, Shinozaki F, Motoyoshi Y, Sugiyama T, Yamamoto S, Ishige N.Int J Oncol. 2016 Jan;48(1):110-4. doi: 10.3892/ijo.2015.3220. Epub 2015 Oct 29. PMID: 26530115 </br>5:FH535 inhibited metastasis and growth of pancreatic cancer cells. Wu MY, Liang RR, Chen K, Shen M, Tian YL, Li DM, Duan WM, Gui Q, Gong FR, Lian L, Li W, Tao M.Onco Targets Ther. 2015 Jul 6;8:1651-70. doi: 10.2147/OTT.S82718. eCollection 2015. PMID: 26185454 Free PMC Article</br>6:FH535 increases the radiosensitivity and reverses epithelial-to-mesenchymal transition of radioresistant esophageal cancer cell line KYSE-150R. Su H, Jin X, Zhang X, Zhao L, Lin B, Li L, Fei Z, Shen L, Fang Y, Pan H, Xie C.J Transl Med. 2015 Mar 31;13:104. doi: 10.1186/s12967-015-0464-6. PMID: 25888911 Free PMC Article</br>7:Targeting the Wnt/β-catenin signaling pathway in liver cancer stem cells and hepatocellular carcinoma cell lines with FH535. Gedaly R, Galuppo R, Daily MF, Shah M, Maynard E, Chen C, Zhang X, Esser KA, Cohen DA, Evers BM, Jiang J, Spear BT.PLoS One. 2014 Jun 18;9(6):e99272. doi: 10.1371/journal.pone.0099272. eCollection 2014. PMID: 24940873 Free PMC Article</br>8:FH535 inhibits the proliferation of HepG2 cells via downregulation of the Wnt/β-catenin signaling pathway. Liu J, Li G, Liu D, Liu J.Mol Med Rep. 2014 Apr;9(4):1289-92. doi: 10.3892/mmr.2014.1928. Epub 2014 Jan 30. PMID: 24482011 </br>9:FH535 inhibited migration and growth of breast cancer cells. Iida J, Dorchak J, Lehman JR, Clancy R, Luo C, Chen Y, Somiari S, Ellsworth RE, Hu H, Mural RJ, Shriver CD.PLoS One. 2012;7(9):e44418. doi: 10.1371/journal.pone.0044418. Epub 2012 Sep 11. PMID: 22984505 Free PMC Article</br>10:FH535 potentiation of cigarette smoke condensate cytotoxicity is associated with changes in β-catenin and EGR-1 signaling. Polk WW.Int J Toxicol. 2012 Jul-Aug;31(4):380-9. doi: 10.1177/1091581812447956. Epub 2012 Jun 19. PMID: 22713211

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