名称 | Jervine |
描述 | The biological activity of Jervine (Jerwiny) is mediated via its interaction with the 7 passes transmembrane protein Smoothened. Jervine binds with and inhibits smoothened, which is an integral part of the Hedgehog signaling pathways. With smoothened inhibited, the GLI1 transcription cannot be activated and Hedgehog target genes cannot be transcribed. |
细胞实验 | Cells are grown in Eagle's basal medium supplemented with 10% fetal bovine serum and 0.25 mg/ml gentamicin sulfate. Cells are seeded onto 35-mm tissue culture plates at a density of 1×104 celldplate. The plated cells are incubated for 24 hours prior to treatment in a humidified incubator at 37 "C in an atmosphere of 5% CO2 in air. Drugs are then added: jervine to a final concentration of 5, 10, or 25 μg/ml; retinoic acid at 0.03, 0.30, or 3.0 pg/ml. After a final 48 hours of incubation, media are removed, the cultures are rinsed three times with phosphate-buffered saline (PBS) pH 7.4, and the cells are harvested into 0.5 ml of 0.1% (w/v) trypsin which contained 0.1% EDTA (w/v) in PBS. Each sample is mixed with 9.5 ml Isoton Ⅱ, and cell numbers are determined by using a Coulter Counter. (Only for Reference) |
体外活性 | Compared to controls, chondrocyte cultures exposed to 25 μg/ml jervine shows an apparent reduction in cell number but no differences in cellular morphology or relative intensity of alcian blue staining[2]. |
体内活性 | Embryos exposed to jervine develop craniofacial abnormalities related to those found in Shh mutant embryos. The lower jaw of these embryos is severely reduced in size, often leading to loss of the incisors. Treatment of pregnant mice with the hedgehog inhibitor jervine induces jaw defects in the embryos similar to those found in Prx1?/?Prx2?/? embryos. The distal part of the jaw is reduced in size, and both incisors are absent[1]. |
存储条件 | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | Chloroform : Soluble H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 5 mg/mL (11.75 mM)
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关键字 | Inhibitor | sterodial | Smoothened | Jervine | rhizomes | antioxidant | Veratrum | album | teratogenic | Hedgehog | alkaloid | anti-inflammatory | Smo | inhibit |
相关产品 | Itraconazole | Naftifine hydrochloride | IHR-1 | GANT 61 | ALLO-2 | Triparanol | LEQ506 | Vismodegib | Halcinonide | MRT-83 | BMS-833923 | Tolnaftate |
相关库 | 抗癌天然产物库 | 生物碱类天然产物库 | 植物来源化合物库 | 天然产物库 | 中药抗炎分子库 | 抑制剂库 | 高通量筛选天然产物库 | 抗衰老化合物库 | 已知活性化合物库 | GPCR靶点分子库 |