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GANT61
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GANT61图片
CAS NO:500579-04-4
规格:98%
分子量:429.6
包装与价格:
包装价格(元)
5mg电议
25mg电议
100mg电议

产品介绍
GLI antagonist
CAS:500579-04-4
分子式:C27H35N5
分子量:429.6
纯度:98%
存储:Store at -20°C

Background:

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 canonical Hedgehog (HH) signaling pathway (SHH->PTCH->SMO-
>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].
参考文献:
[1].Wang, J., et al., Inhibition of autophagy potentiates the efficacy of Gli inhibitor GANT-61 in MYCN-amplified neuroblastoma cells. BMC Cancer, 2014. 14: p. 768.
[2].Agyeman, A., et al., Mode and specificity of binding of the small molecule GANT61 to GLI determines inhibition of GLI-DNA binding. Oncotarget, 2014. 5(12): p. 4492-503.
[3].Srivastava, R.K., et al., GLI inhibitor GANT-61 diminishes embryonal and alveolar rhabdomyosarcoma growth by inhibiting Shh/AKT-mTOR axis. Oncotarget, 2014. 5(23): p. 12151-65.