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FH535 CAS: 108409-83-2

Category: Inhibitors
Product Name: FH535
Cat No: I000367
CAS No: 108409-83-2
Synonyms: 2,5-dichloro-N-(2-methyl-4-nitrophenyl)benzenesulfonamide
Molecular Formula: C13H10Cl2N2O4S
Molecular Weight: 361.2
SMILES: ClC1=C(S(NC2=C(C)C=C([N+]([O-])=O)C=C2)(=O)=O)C=C(Cl)C=C1
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
Solubility: DMSO: > 10 mM
Target: Wnt/β-catenin
IC50: 1.1 uM (Cytotoxicity in the CCLP-1 cell line) [1]
Storage: Store at -20°C
CAS 108409-83-2,FH535
  • Description

FH535 is a compound that suppresses both Wnt/beta-catenin and peroxisome proliferator-activated receptor (PPAR) signaling.
IC50 Value: 1.1 uM (Cytotoxicity in the CCLP-1 cell line) [1]
Target: PPAR; Wnt/beta-catenin
FH535antagonizes both PPAR gamma and PPAR delta ligand-dependent activation and shows structural similarity to GW9662, a known PPAR gamma antagonist.
in vitro: FH535 significantly inhibited cell migration of Mel 1241 cells, which was associated with the elevated levels of casein kinase 1α and glycogen synthase kinase-3β, and decreased accumulation of nuclear β-catenin and inhibition of MMP-2 and MMP-9 levels [2]. FH535 was shown to increase CSC-induced cytotoxicity and depress β-catenin expression. However, FH535 effects were not limited to the β-catenin pathway as it also blocked the expression of early growth responsive protein 1 (EGR-1) target genes, fibronectin and phosphatase and tensin homologue, without affecting EGR-1 nuclear accumulation [3]. Western blotting analyses suggest that treatment of MDA-MB-231 cells with FH535 markedly inhibited the expression of NEDD9 but not activations of FAK, Src, or downstream targets such as p38 and Erk1/2 [4].
in vivo:

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


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
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
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
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
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
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
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
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
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
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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