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GANT 58

GANT 58

产品编号 T15370   CAS 64048-12-0
别名: 4,44乔,4乔(2,3,4,5-Thiophentetrayl)tetrakis-pyridine, NSC 75503

GANT 58 (NSC-75503) 是GLI 拮抗剂,能够抑制 GLI1 诱导的转录,其IC50=5 μM。

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GANT 58 Chemical Structure
GANT 58, CAS 64048-12-0
规格 价格/CNY 货期 数量
2 mg ¥ 263 现货
5 mg ¥ 413 现货
10 mg ¥ 676 现货
25 mg ¥ 1,330 现货
50 mg ¥ 2,470 现货
100 mg ¥ 3,990 现货
1 mL * 10 mM (in DMSO) ¥ 466 现货
千万补贴 助力科研
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Doxorubicin hydrochloride限时半价
产品目录号及名称: GANT 58 (T15370)
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生物活性
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存储 & 溶解度
参考文献
产品描述 GANT 58 (NSC-75503) is a potent antagonist of Gli. Which inhibits GLI1-induced transcription (IC50: 5 μM).
靶点活性 GLI:5 μM
体外活性 GANT58 is a downstream inhibitor of Hh signaling and it also is an indeed inhibitor of Hh signaling downstream of Smo and Sufu. GANT58 potently inhibits in vitro tumor cell proliferation in a GLI-dependent manner and successfully blocks cell growth using human prostate cancer cells harboring downstream activation of the Hh pathway[1]. GANT58 has been shown to inhibit transcriptional activation by GLI1 (as well as by the other GLI species) and it has been shown to inhibit GLI transactivation[2]. GANT58 mainly acts at the nuclear level because transcription induced by GLI1 with a mutated nuclear export signal is still blocked.
体内活性 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[1].
别名 4,44乔,4乔(2,3,4,5-Thiophentetrayl)tetrakis-pyridine, NSC 75503
分子量 392.48
分子式 C24H16N4S
CAS No. 64048-12-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 9.09 mg/mL (23.16 mM), Sonication is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5479 mL 12.7395 mL 25.479 mL 63.6975 mL
5 mM 0.5096 mL 2.5479 mL 5.0958 mL 12.7395 mL
10 mM 0.2548 mL 1.274 mL 2.5479 mL 6.3698 mL
20 mM 0.1274 mL 0.637 mL 1.274 mL 3.1849 mL

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TargetMol Library Books参考文献

1. 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. 2. Joo J, et al. GLI1 is a central mediator of EWS/FLI1 signaling in Ewing tumors. PLoS One. 2009 Oct 27;4(10):e7608.
Dynarrestin MK-4101 GSA-10 BMS-833923 Purmorphamine Ciliobrevin D Vismodegib HhAntag

相关化合物库

该产品包含在如下化合物库中:
GPCR靶点分子库 膜蛋白靶向化合物库 抑制剂库 干细胞分化化合物库 抗前列腺癌化合物库 已知活性化合物库 Wnt/Hedgehog/Notch 通路化合物库 经典已知活性库 细胞重编程化合物库 成骨分子库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

GANT 58 64048-12-0 GPCR/G Protein Stem Cells Hedgehog/Smoothened inhibit Inhibitor GANT58 GANT-58 Gli NSC75503 NSC-75503 4,44乔,4乔(2,3,4,5-Thiophentetrayl)tetrakis-pyridine NSC 75503 inhibitor

 

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