Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GANT 61 (GANT61) 是一种Gli1和Gli2抑制剂,靶向Hedgehog/GLi 通路。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 238 | 现货 | ||
2 mg | ¥ 335 | 现货 | ||
5 mg | ¥ 537 | 现货 | ||
10 mg | ¥ 855 | 现货 | ||
25 mg | ¥ 1,730 | 现货 | ||
50 mg | ¥ 3,390 | 现货 | ||
100 mg | ¥ 4,760 | 现货 | ||
500 mg | ¥ 9,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 539 | 现货 |
产品描述 | GANT 61 (GANT61) is an inhibitor for Gli1 and Gli2. |
靶点活性 | GLI1:5 μM |
体外活性 | 携带SK-N-AS神经母细胞瘤移植瘤的裸鼠口服饲喂50 mg/kg GANT61,在实验第12天明显抑制肿瘤生长,与对照组相比,肿瘤体积减少63%.在注射GLI1阳性22Rv1前列腺癌细胞的裸鼠中,GANT61诱导肿瘤生长退化,直到观察不到明显的肿瘤. |
体内活性 | GANT61以GLI依赖性方式有效抑制体外肿瘤细胞增殖。30 μM GANT61导致急性髓系白血病细胞生长停滞和凋亡。GANT61对人结肠癌细胞系具有强大的细胞毒性,且消除集落生成。GANT61作用于慢性淋巴细胞性白血病细胞,而非正常的B淋巴细胞,诱导细胞凋亡。GANT61在人结肠癌细胞系的早期S期中诱导DNA复制的抑制,导致ATM-Chk2轴的DNA损伤信号传导和诱导细胞死亡。GANT61抑制GLI1的DNA结合能力。GANT61抑制hedgehog信号,IC50为5 μM,比作用于其他通路选择性高(如TNF信号/NFκB激活,糖皮质激素受体基因转录,及Ras-Raf-Mek-Mapk级联)。 |
激酶实验 | Dual Luciferase Assay: HEK293 cells are transfected with GLI1 expression plasmid, together with the reporter plasmids 12×GliBSLuc and R-Luc on 10-cm plates (day 0). Twenty-four hours later, cells are seeded in white 96-well plates with clear bottom at a density of 15,000 cells per well. Cells are allowed to attach, and compounds are added at a final concentration of 10 μM in DMSO (0.5% final DMSO concentration) (day 1.5). Cells are grown for another 24 h, subsequently lysed, and then analyzed by using the Dual Luciferase kit. |
细胞实验 | BrdU Incorporation Assay. Subconfluent cells are grown in reduced FBS (2.5%) for 48 h in the presence of 5 μM test compound (or DMSO) on white 96-well plates with clear bottom. Subsequently, cells are labeled for 2 h with BrdU, fixed, and analyzed.(Only for Reference) |
别名 | NSC 136476, GANT61 |
分子量 | 429.6 |
分子式 | C27H35N5 |
CAS No. | 500579-04-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 4.3 mg/mL (10 mM), Sonication is recommended.
Ethanol: 43 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.3277 mL | 11.6387 mL | 23.2775 mL | 58.1937 mL |
5 mM | 0.4655 mL | 2.3277 mL | 4.6555 mL | 11.6387 mL | |
10 mM | 0.2328 mL | 1.1639 mL | 2.3277 mL | 5.8194 mL | |
Ethanol | 20 mM | 0.1164 mL | 0.5819 mL | 1.1639 mL | 2.9097 mL |
50 mM | 0.0466 mL | 0.2328 mL | 0.4655 mL | 1.1639 mL | |
100 mM | 0.0233 mL | 0.1164 mL | 0.2328 mL | 0.5819 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
GANT 61 500579-04-4 Autophagy GPCR/G Protein Stem Cells Hedgehog/Smoothened NSC 136476 Inhibitor Gli GANT-61 NSC-136476 GANT61 NSC136476 inhibit inhibitor