| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| S408954-1ml |
1ml |
现货  |
|
| 英文别名 | TCS PIM-1 4a | 2,4-Thiazolidinedione, 5-[[3-(trifluoromethyl)phenyl]methylene]-, (5Z)- |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | SMI-4a |
| 生化机理 | SMI-4a （TCS PIM-1 4a）是一种 17 nM 的强效抑制剂，对 Pim-2 有一定的抑制作用，但对其他丝氨酸/苏氨酸或酪氨酸激酶没有明显的抑制作用。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
SMI-4a是一种有效的Pim1抑制剂，IC50为17 nM，作用于Pim-2适度有效，抑制其他丝/苏氨酸或酪氨酸激酶作用不显著。A selective and ATP-competitive Pim kinase inhibitor Information SMI-4a (TCS PIM-1 4a) is a potent inhibitor of Pim1 with IC50 of 17 nM, modestly potent to Pim-2, does not significantly inhibit any other serine/threonine- or tyrosine-kinases. SMI-4a is an ATP competitive inhibitor of Pim1 with IC50 of 17 nM. SMI-4a shows high selectivity for Pim1 against a panel of kinases. SMI-4a inhibits the in vitro phosphorylation by Pim-1 of the known substrate, the translational repressor 4E-BP1. SMI-4a (5μM) inhibits pancreatic and leukemic cells growth. SMI-4a reduces phosphorylation of the Pim target Bad in prostate and hematopoietic cells. SMI-4a causes cell cycle arrest and reverses the antiapoptotic activity of Pim-1. SMI-4a increases the amount of p27Kip1 in the nucleus. SMI-4a treatment of pre-T-LBL inhibits the mTOR pathway. SMI-4a reduces MYC protein expression in pre-T-LBL. SMI-4a treatment induces up-regulation of MAPK pathway. In vivo SMI-4a (60 mg/Kg) treatment twice daily significantly reduce tumor size and is well tolerated. Tumors harvested 1 hour after the final oral gavage of SMI-4a demonstrates decreased phosphorylation of p70 S6K compared with tumors from mice treated with vehicle, whereas in comparison total p70 S6K expression isunchanged. cell lines： Concentrations： Incubation Time： Powder Purity:≥97% |
| IC50 | Pim1, IC50: 17 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | FC(F)(F)C1=CC(=CC=C1)\C=C2/SC(=O)NC2=O |
| 分子量 | 273.23 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 100 mg/mL (406.07 mM); |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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