GlpBio

FH535

目录号: GC12134纯度: >99.50%同义词: 2,5-二氯-N-(2-甲基-4-硝基苯基)苯磺酰胺,FH 535;FH-535
An inhibitor of β-catenin signaling
FH535
Cas No.: 108409-83-2
规格价格库存数量操作
10mg¥462.00现货
1
50mg¥1,323.00现货
1
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文献被引

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    641, 529–536 (2025)
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    628, 630–638 (2024)
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    632, 686–694 (2024)
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    618, 1017–1023 (2023)
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    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    388(6745) (2025)
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    387(6739) (2025)
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    387(6734) (2025)
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    35, 97–116 (2025)
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    33, 546–561 (2023)
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    33, 904–922 (2023)
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    31, 1291–1307 (2021)

产品描述 Description

FH535 is a small molecule inhibitor of Wnt/B-catenin with IC50 values of 15.4μM, 10.9μM, 9.3μM, respectively in LCSC, Huh7, PLC cell lines [1].

FH535 can inhibit the growth of colon, lung, and hepatocellular carcinoma line but not normal fibroblasts. It makes FH535 potentially be a promising therapeutic approach for cancer cells. It is reported that FH535 has ability to inhibit growth, migration, and invasion of TN breast cancer cell lines (MDA-MB-231 and HCC38) without affecting adhesive abilities of cells to type I collagen [2].

FH535 is also an inhibitor of peroxisome proliferator–activated receptor (PPAR). It plays a role as a dual PPARγ and PPARδ antagonist that is able to inhibit GRIP1 and β-catenin recruitment [3].

References:
[1] Roberto R. Galuppo, Roberto Gedaly, Paul Angulo, Michael F. et al. FH535 inhibits wnt/β-catenin signaling pathway in liver cancer stem cells and HCC cell lines. Hepatology. 2013, October: 466A.
[2] Joji Iida, Jesse Dorchak, John R. Lehman, Rebecca Clancy, Chunqing Luo, Yaqin Chen, Stella Somiari, Rachel E. Ellsworth, Hai Hu, Richard J. Mural, Craig D. Shriver. FH535 Inhibited Migration and Growth of Breast Cancer
Cells. PLOS ONE. 2012, 7(9): 1-11.
[3] Shlomo Handeli and Julian A. Simon. A small-molecule inhibitor of Tcf/β-catenin signaling down-regulates PPARγ and PPARδ activities. Molecular Cancer Therapeutics. 2008, 7:521-529.

实验参考方法 Experimental Reference Method

Kinase experiment [1]:

High-throughput library screen

Three copies of the optimized or mutated Tcf-binding element from TOPFLASH or FOPFLASH driving a secreted alkaline phosphatase reporter gene were cloned into pCEP4 plasmid, replacing the cytomegalovirus promoter. The plasmids were transfected into HepG2 cells, and Hygromycin-resistant clones were pooled. Library screening was done at 20 μmol/L concentration in HepG2 serum-free media. Hits were tested in the HCT116 cell line for inhibition of TOPFLASH luciferase activity but not for inhibition of a reporter activity controlled from β-actin promoter.
Cell experiment [1]:

Cell lines

HCT116, SW48, RKO, LoVo, COLO205, IEC6, A427, HCC15, NCI-H1703, A549, HepG2, Hep3b, Huh7 and fibroblasts

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

30 μM; 48 hrs

Applications

FH535 showed selective anti-proliferation effect on some cancer cells (HCT116, SW48, RKO, LoVo, COLO205, A427, HCC15, NCI-H1703, A549, HepG2, Hep3b and Huh7 cells) expressing high or active Wnt/β-catenin pathway.
Animal experiment [2]:

Animal models

Nude mouse bearing pancreatic cancer xenografts

Dosage form

25 mg/kg; i.p.; every 2 days for 20 days

Applications

FH535 significantly repressed pancreatic cancer xenograft growth in vivo and showed better performance status with respect to body weight loss.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Shlomo Handeli and Julian A. Simon. A small-molecule inhibitor of Tcf/β-catenin signaling down-regulates PPARγ and PPARδ activities. Molecular Cancer Therapeutics. 2008, 7:521-529.

[2]. 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 Jun 13.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
108409-83-2
同义词
2,5-二氯-N-(2-甲基-4-硝基苯基)苯磺酰胺,FH 535;FH-535
化学名
2,5-dichloro-N-(2-methyl-4-nitrophenyl)benzenesulfonamide
SMILES
CC1=C(C=CC(=C1)[N+](=O)[O-])NS(=O)(=O)C2=C(C=CC(=C2)Cl)Cl
分子式
C13H10Cl2N2O4S
分子量
361.2 g/mol
溶解性
≥ 36.1 mg/mL in DMSO, ≥ 5.87 mg/mL in EtOH with gentle warming
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol