GFH018 methylbenzenesulfonate 

GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC₅₀ of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma^[1].

GFH018 (0.2 nM-40 μM; 40 min) methylbenzenesulfonate inhibits p38α enzymatic activity with an IC₅₀ of 2,648 nM, and is 66.2-fold more selective for TGF-βR1 than for p38α^[1].
GFH018 methylbenzenesulfonate inhibits the proliferation of NIH 3T3 fibroblasts with an IC₅₀ of 0.73 μM^[1].
GFH018 methylbenzenesulfonate inhibits TGF-β-induced Smad phosphorylation in HEK293 reporter cells, with an IC₅₀ of 105 nM^[1].
GFH018 (0.1-10 μM; 4 days) methylbenzenesulfonate dose-dependently inhibits TGF-β-induced Treg differentiation in a mouse CD4⁺ T cell-APC co-culture system, with the strongest inhibitory effect observed at the concentration of 10 μM^[1].
GFH018 (0.1-10 μM; 16 h) methylbenzenesulfonate regulates cytokine secretion in human M2 macrophages in a dose-dependent manner, upregulating TNF-α and IL-6 levels while downregulating IL-10 levels at concentrations ranging from 0.1 to 10 μM^[1].
GFH018 (0.1-10 μM; 6 h) methylbenzenesulfonate inhibits tube formation of HUVEC cells on Matrigel in a dose-dependent manner. After 6 h of incubation, significant reductions in the number of nodes and tube length are observed at concentrations ranging from 0.1 to 10 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GFH018 (15-50 mg/kg; p.o.; twice daily; for 11 consecutive days) methylbenzenesulfonate exhibits dose-dependent in vivo anti-tumor activity in a mouse liver cancer model^[1].
GFH018 (50 mg/kg; p.o.; twice daily) methylbenzenesulfonate and anti-PD-L1 antibody exerts synergistic antitumor efficacy in a mouse colorectal cancer model, with a TGI of 79.4%^[1].
GFH018 (100 mg/kg; p.o.; twice daily; for 32 days) methylbenzenesulfonate potently inhibits the metastasis of breast cancer to multiple organs in vivo at an oral dose of 100 mg/kg twice daily^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

557.62

C₂₈H₂₇N₇O₄S

2345717-52-2

NC(/C=C/C1=C(C=CC2=NC=NN21)C3=C(CCC4)N4N=C3C5=CC=CC(C)=N5)=O.O=S(O)(C6=CC=C(C=C6)C)=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Jiang T, et al. Discovery of a Selective, Novel TGF-βR1 Inhibitor GFH018 for the Treatment of Solid Tumors. J Med Chem. 2025;68(12):12513-12530.