| 名称 | GANT 61 |
| 描述 | GANT 61 (GANT61) is an inhibitor for Gli1 and Gli2. |
| 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) |
| 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. |
| 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）。 |
| 存储条件 | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 25 mg/mL (58.19 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.33 mM), Sonication is recommended.
Ethanol : 43 mg/mL (100.09 mM), Sonication is recommended.
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| 关键字 | Smoothened | NSC-136476 | NSC136476 | Inhibitor | inhibit | Hedgehog | GLI1 | Gli | GANT-61 | GANT 61 | Autophagy |
| 相关产品 | Naringin | Guanidine hydrochloride | Gefitinib | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Hemin | Hydroxychloroquine | Stavudine | Tamoxifen | Paeonol | Sodium 4-phenylbutyrate |
| 相关库 | 抑制剂库 | 经典已知活性库 | 已知活性化合物库 | 抗衰老化合物库 | 干细胞分化化合物库 | 抗肥胖化合物库 | 血液病分子库 | GPCR靶点分子库 | 膜蛋白靶向化合物库 | 神经元分化化合物库 | Wnt/Hedgehog/Notch 通路化合物库 | 细胞重编程化合物库 |