Drug intelligence / Profile preview

GANT61

Development stage
Preclinical
Modality
Small Molecules
Administration
Not Applicable (preclinical/research Use; Used Primarily In Vitro And In Vivo In Animal Models)
01

Overview

GANT61 is a **synthetic small-molecule inhibitor** that selectively targets **GLI transcription factors (GLI1 and GLI2)** in the **Hedgehog signaling pathway** by direct binding and blocking their DNA binding ability, thereby suppressing their transcriptional activity[1][4][5][8]. It inhibits cancer cell proliferation and induces apoptosis, often in a caspase-independent manner, across a variety of cancer cell types including Ewing's sarcoma, hepatocellular carcinoma, colorectal cancer, and T-cell lymphoma[1][3][4][6][7]. GANT61 also blocks the **Wnt/β-catenin** and **Notch signaling pathways**, affecting cancer stem cell viability and the malignant behavior of tumor cells[3][7]. The compound is primarily used in preclinical research settings due to its role as an antineoplastic and apoptosis inducer, and has not been approved for clinical use.

Brand names
GANT61GANT-61GANT 61
Other names
2,2'-((2-(pyridin-4-yl)dihydropyrimidine-1,3(2H,4H)-diyl)bis(methylene))bis(N,N-dimethylaniline)2-[[3-[[2-(dimethylamino)phenyl]methyl]-2-pyridin-4-yl-1,3-diazinan-1-yl]methyl]-N,N-dimethylaniline
02

Targets

GLI2

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