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Wnt&Beta catenin

FH535 (108409-83-2)

FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.

Not Intended for Therapeutic Use. For research use only.

CAS: 108409-83-2 Category

FH535 (108409-83-2) Description

β-Catenin/Tcf Inhibitor, FH535 is a sulfonamide-based and cell-permeable compound that exhibits a dual pathway inhibition against Wnt/β-catenin and PPAR. FH535 and its structurally similar analog, PPAR inhibitor GW9662, both exhibit inhibition of coactivator/PPAR binding, though only FH535 blocks β-catenin/PPAR interaction. Further, the antagonistic activity of FH535 does not involve the covalent modification of non-covalent interaction with the PPR ligand-binding site cysteine residue, which has been experimentally shown to be crucial for GW9662 action. β-Catenin/Tcf Inhibitor, FH535 is an inhibitor of GRIP1, PPAR-β, and PPAR-γ.

 

FH535 (108409-83-2) Specifications

Product Name FH535
Synonyms FH535; FH 535; FH-535
Chemical Names 2,5-dichloro-N-(2-methyl-4-nitrophenyl)-benzenesulfonamide
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 108409-83-2
Molecular Formula C13H10Cl2N2O4S
Molecular Weight 361.193
Monoisotopic Mass 359.974 g/mol
MDL number MFCD01212888
InChIKey AXNUEXXEQGQWPA-UHFFFAOYSA-N
InChi Code 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
SMILES O=S(C1=CC(Cl)=CC=C1Cl)(NC2=CC=C([N+]([O-])=O)C=C2C)=O
Form Powder
Color Off-white
Solubility  Soluble in DMSO, not in water
Storage Temp.  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
Handling Protect from air and light
Application A cell-permeable compound that inhibits Wnt/β-catenin and PPAR

 


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RIDADR NONH for all modes of transport

References:

  • 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.