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.
Chemical Formula: C13H10Cl2N2O4S
Exact Mass: 359.9738
Molecular Weight: 361.193
Elemental Analysis: C, 43.23; H, 2.79; Cl, 19.63; N, 7.76; O, 17.72; S, 8.88
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
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).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
FH535 is an inhibitor of Wnt/β-catenin and PPAR. FH535 inhibits PPARγ and PPARδ transactivation in HCT116 cells. FH535 (15 μM) activities depend on functional PPARδ but does not require a cysteine residue in the PPAR ligand-binding domain. FH535 inhibits recruitment of the coactivators GRIP1 and β-catenin to PPARδ and PPARγ. FH535 shows toxic effects on 12 carcinoma cell lines expressing wnt/β-catenin pathway. FH535 (20 μM) suppresses the β-catenin pathway in pancreatic cancer cells, and inhibits pancreatic cancer cell migration. Furthermore, FH535 (20, 40 μM) inhibits pancreatic cancer cell invasion and cell growth. FH535 represses angiogenesis-related genes in pancreatic cancer cells.
FH535 (25 mg/kg, i.p.) exhibits an anti-tumor effect on pancreatic cancer xenografts in mice. FH535 also represses angiogenesis in pancreatic cancer xenografts.
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.
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.
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.
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.
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.
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