Mitogen activated protein kinase interacting kinase; MAP kinase interacting kinase; MAPK interacting kinase
Mitogen-activated protein kinase-interacting kinases 1 and 2 (MNK1 and MNK2) phosphorylate the oncogene eIF4E on serine 209. This phosphorylation has been reported to be required for its oncogenic activity. Eukaryotic initiation factor 4E (eIF4E) is a key component of the translational machinery and an important modulator of cell growth and proliferation. The activity of eIF4E is thought to be regulated by interaction with inhibitory binding proteins (4E-BPs) and phosphorylation by mitogen-activated protein (MAP) kinase-interacting kinase (MNK) on Ser209 in response to mitogens and cellular stress.
货号 | 产品名 | Cas | 产品描述 |
---|---|---|---|
PL07434 | DS12881479 | 2373065-59-7 | DS12881479 是一种有效的选择性 Mnk1 抑制剂,其 IC50 值为21 nM. DS12881479 可用于癌症研究。 |
PL07435 | SLV-2436 | 2095704-43-9 | SLV-2436 是一种高效且 ATP 竞争性的 MNK1 和 MNK2 抑制剂,IC50 分别为 10.8 nM 和 5.4 nM。 |
PL07436 | Tinodasertib | 1464151-33-4 | Tinodasertib (ETC-206) 是一种选择性 MNK1 和 MNK2 抑制剂,IC50 分别为 64 nM 和 86 nM。 |
PL07437 | Tomivosertib | 1849590-01-7 | Tomivosertib (eFT508) 是一种有效的,高度选择性的,口服活性的 MNK1 和 MNK2 抑制剂,IC50 值均为 1-2 nM。Tomivosertib (eFT508) 处理可降低肿瘤细胞中 eIF4E 的磷酸化水平 (位点为 Ser209,IC50=2-16 nM)。Tomivosertib (eFT508) 还显著下调 PD-L1 蛋白的丰度。 |