| 名称 | Sepantronium bromide |
| 描述 | Sepantronium bromide (YM155) is a small-molecule proapoptotic agent with potential antineoplastic activity. |
| 细胞实验 | Cells are seeded in 96-well plates at a density of 5-40 × 103. YM155 is dissolved in DMSO and added to cells for 48 hours. Then the cell count is determined by sulforhodamine B assay. (Only for Reference) |
| 激酶实验 | Promoter-luciferase reporter assay: A 2,767-bp sequence of human survivin gene promoter is isolated from human genomic DNA by PCR using Pyrobest polymerase and the following primers: 5 |
| 体外活性 | YM155有效抑制人类癌细胞系(突变p53或短小p53) 包括PC-3,PPC-1,DU145,TSU-Pr1,22Rv1,SK-MEL-5及A375,IC50值为2.3到11 nM。YM155显著抑制具有缺陷p53的PC-3和PPC-1人HRPC细胞中的内源性存活蛋白表达。相反,YM155在100 nM对c-IAP2,XIAP,Bcl-2,Bcl-xL,Bad,α-肌动蛋白和β-微管蛋白的蛋白质表达无明显影响。YM155诱导包括PC-3和PPC-1在内的人类癌细胞系大量凋亡,伴随着胱天蛋白酶-3活性增加。另外,YM155增强NSCLC细胞对γ-射线的敏感性。YM155和γ-射线联用,增强凋亡细胞数和caspase-3活性。 |
| 体内活性 | 皮下注射3和10 mg/kg YM155到前列腺移植瘤,结果显示YM155完全抑制PC-3的肿瘤生长,且重量没有降低,血细胞数也没有下降.而且,在PC-3常位移植瘤中,5 mg/kg YM155对肿瘤抑制率达80%.YM155和γ-射线联用在裸鼠体内显示出对抗H460或Calu6异种移植物的高抗肿瘤活性. |
| 存储条件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.26 mM), Sonication is recommended.
H2O : 82 mg/mL (184.99 mM), Sonication is recommended.
Ethanol : 6 mg/mL (13.54 mM), Sonication is recommended.
DMSO : 48 mg/mL (108.29 mM), Sonication is recommended.
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| 关键字 | YM-155 | YM 155 | Survivin | Sepantronium bromide | Sepantronium | Inhibitor | inhibit | Autophagy |
| 相关产品 | Guanidine hydrochloride | Naringin | Enzalutamide | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Hemin | Hydroxychloroquine | Stavudine | Tamoxifen | Paeonol | Sodium 4-phenylbutyrate |
| 相关库 | 抑制剂库 | 抗乳腺癌化合物库 | 抗癌活性化合物库 | 经典已知活性库 | 抗癌化合物库 | 已知活性化合物库 | 细胞凋亡化合物库 | 抗衰老化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库 | 抗前列腺癌化合物库 |