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GANT61 is a selective inhibitor of GLI with IC50 value of 13.56 μM (NBL-W-S cells, 48 hours) [1].

GLI genes, GLI1 and GLI2, are transcription activator and regulate target genes at the distal end of the

>GLI). It is well known that HH signaling plays a pivotal role in normal cellular processes, like embryonic development, tissue patterning and differentiation. As oncogenes, GLI1 and GLI2 are found to be constitutively activated in a variety types of human cancers [2].

GANT61 is a potent GLIs inhibitor. In SK-N-EB(2) cells expressing MYCN, GANT61 treatment reduced the cell viability with the IC50 value of 10.9μM and 7.96μM at 48 hours and 72 hours, respectively [1]. When tested with human RMS cell lines—RD and RH30, GANT-61 treatment exhibited anti-proliferative effects and induced cell death in a dose-dependent manner (5-25 μM) via decreasing GLI1/2 expression which resulted in the arrest of cell cycle at Go/G1 phase [3].

In nude mice model with RD or RH30 cells xenograft, intraperitoneal injected GANT-61 (50mg/kg, body weight in 200μl PBS; three times a week) markedly reduced tumor growth [3].

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