| Description | (Z)-SMI-4a (TCS PIM-1 4a) is a selective ATP-competitive Pim-1 kinase inhibitor with an IC50 of 21 nM. |
| In vitro | 口服SMI-4a后1小时,与对照组小鼠肿瘤相比,p70 S6K磷酸化减少,而总的p70 S6K表达不变.每天60 mg/kg SMI-4a处理两次,明显降低肿瘤尺寸,且具有良好的耐受性. |
| In vivo | 5 μM SMI-4a抑制胰腺癌和白血病细胞生长。SMI-4a降低前列腺和造血细胞中Pim靶点的磷酸化。SMI-4a引起细胞周期停滞并逆转Pim-1的抗凋亡活性。SMI-4a是Pim1的ATP竞争性抑制剂,IC50为17 nM。SMI-4a显示Pim1对一组激酶具有高选择性。SMI-4a抑制已知底物即翻译阻遏物4E-BP1的Pim-1的体外磷酸化。SMI-4a增加细胞核中p27Kip1的量。SMI-4a处理诱导MAPK通路上调。SMI-4a处理pre-T-LBL,抑制mTOR通路。 |
| Target activity | Pim1:21 nM |
| Synonyms | TCS PIM-1 4a, SMI-4a |
| molecular weight | 273.23 |
| Molecular formula | C11H6F3NO2S |
| CAS | 438190-29-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: 27.3 mg/mL (100 mM) DMSO: 65 mg/mL (237.89 mM), Sonication is recommended. |
| References | 1. Beharry Z, et al. Mol Cancer Ther, 2009, 8(6), 1473-1483. 2. Lin YW, et al. Blood, 2010, 115(4), 824-833. |