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干细胞
Notch Hedgehog (Hh)
/ Gli / GANT 58

GANT 58 {[allProObj[0].p_purity_real_show]}

货号：A430364 同义名： NSC 75503 Ambeed 开学季，买赠积分，赢豪礼

GANT 58 is a potent Gli antagonist that inhibits GLI1-induced transcription (IC50 = 5 μM).

GANT 58 化学结构 CAS号：64048-12-0
GANT 58 化学结构
CAS号：64048-12-0
GANT 58 3D分子结构
CAS号：64048-12-0
GANT 58 化学结构 CAS号：64048-12-0
GANT 58 3D分子结构 CAS号：64048-12-0
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GANT 58 纯度/质量文件 产品仅供科研

货号：A430364 标准纯度： {[allProObj[0].p_purity_real_show]}
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GANT 58 生物活性

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].

GANT 58 参考文献

[1]Joo J, Christensen L, et al. GLI1 is a central mediator of EWS/FLI1 signaling in Ewing tumors. PLoS One. 2009 Oct 27;4(10):e7608.

[2]Lauth M, Bergstrom A, et al. Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8455-60. Epub 2007 May 9.

[3]Prasuja Rokkam,et al. Prognostic Role of Hedgehog-GLI1 Signaling Pathway in Aggressive and Metastatic Breast Cancers. Curr Drug Metab. 2020;21(1):33-43.

[4] Joo J, et al. GLI1 is a central mediator of EWS/FLI1 signaling in Ewing tumors. PLoS One. 2009 Oct 27;4(10):e7608.

[5] Lauth M, et al. Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8455-60.

[6]Ji Zhu,et al. Regulation of angiogenic behaviors by oxytocin receptor through Gli1-indcued transcription of HIF-1α in human umbilical vein endothelial cells. Biomed Pharmacother. 2017 Jun;90:928-934.

GANT 58 实验方案

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

GANT 58 技术信息

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

Tags: GANT 58 | NSC 75503 | Gli | AmBeed-信号通路专用抑制剂 | GANT 58 纯度/质量文件 | GANT 58 生物活性 | GANT 58 参考文献 | GANT 58 实验方案 | GANT 58 技术信息

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