GANT 58 is a potent Gli antagonist that inhibits GLI1-induced transcription (IC50 = 5 μM).
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描述 | Glioma-associated oncogene homolog 1 (GLI1) is an amplified gene in human glioblastoma cells. It is a krupple like transcription factor, belonging to the zinc finger family. The basic function of GLI1 is normal neural development at various stages of human[3].GANT58 (NSC75503) has been shown to inhibit transcriptional activation by GLI1 (as well as by the other GLI species). GANT58 has been shown to inhibit GLI transactivation[4].GANT 58 (NSC 75503) is a potent GLI antagonist that inhibits GLI1-induced transcription with IC50 of 5 μM. Nude mice are treated with every second-day s.c. injections at a concentration of 50 mg/kg of cyclopamine, GANT61, GANT58, or solvent only (n=4-5 for each group). Although mice treated with these compounds showed no such signs of toxicity, this protocol is also introduced for the GANTs to be able to compare all compounds. All injections are done 2-3 cm away from the tumors. Suppression of tumor cell growth is observed for all compounds, during an 18-day treatment period. Treatment with cyclopamine or GANT58 results in the inhibition of additional xenograft growth and limited the increase in tumor size[5].GANT-58 at 5μM significantly abolished oxytocin-induced mRNA and protein expression of HIF-1α, while the nuclear abundance of Gli1 was significantly reduced by atosiban at 10μM, but was increased by oxytocin at 0.1μM in human umbilical vein endothelial cells(HUVECs). GANT-58 at 5μM also significantly abolished oxytocin-enhanced angiogenic properties of HUVECs[6]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.55mL 0.51mL 0.25mL |
12.74mL 2.55mL 1.27mL |
25.48mL 5.10mL 2.55mL |
CAS号 | 64048-12-0 |
分子式 | C24H16N4S |
分子量 | 392.476 |
别名 | NSC 75503 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 8 mg/mL(20.38 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 无水乙醇: 20 mg/mL(50.96 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇 |
动物实验配方 |