MNK

特异性亚型抑制剂

• MNK1 Selective
• MNK2

MNK产品

目录号	产品描述	文献引用	实验数据
S6658	ETC-206 (AUM 001) ETC-206 (AUM 001, ETC-1907206)是一种可口服、高选择性的MNK 1/2抑制剂，IC50分别为64 nM和86 nM。
S7421	CGP 57380 CGP 57380 是强效的MNK1抑制剂，其IC50为 2.2 μM,对 p38, JNK1, ERK1 和 -2, PKC, 或 c-Src-like kinases显示无抑制活性。CGP 57380 可上调 β-catenin 并加强辐射诱导的凋亡。	Fundam Clin Pharmacol, 2022, 10.1111/fcp.12759 J Cancer, 2020, 11(4):990-996 Bioorg Med Chem, 2018, 26(16):4602-4614	PC-3 cells were seeded in 6-well plates. On the next day, cells were treated with the indicated concentrations of 3-AWA, LY294002, CGP57380 or Rapamycin alone and or combination for 12 h. The cells were then subjected to preparation of whole-cell lysates for detection of the indicated proteins using western blotting. The western blots are the representative of three similar experiments.
S6888	SEL201 SEL-201 (SLV-2436, SEL201-88) 是一种高效的、ATP竞争性的 MNK1 和 MNK2 的抑制剂，对应的IC50值分别为10.8 nM和5.4 nM。
S8275	Tomivosertib (eFT-508) Tomivosertib (eFT-508) 是一种有效的、选择性的MNK1/2的抑制剂，IC50分别为2.4 nM和1 nM。它能减少肿瘤细胞的增殖和肿瘤生长。Tomivosertib (eFT-508) 可抑制 eIF4E 磷酸化并显着下调 PD-L1 蛋白质的丰度。	J Med Chem, 2022, 10.1021/acs.jmedchem.1c01941 Fundam Clin Pharmacol, 2022, 10.1111/fcp.12759 J Clin Invest, 2021, 140752

目录号	产品描述	文献引用	实验数据
S6658	ETC-206 (AUM 001) ETC-206 (AUM 001, ETC-1907206)是一种可口服、高选择性的MNK 1/2抑制剂，IC50分别为64 nM和86 nM。
S7421	CGP 57380 CGP 57380 是强效的MNK1抑制剂，其IC50为 2.2 μM,对 p38, JNK1, ERK1 和 -2, PKC, 或 c-Src-like kinases显示无抑制活性。CGP 57380 可上调 β-catenin 并加强辐射诱导的凋亡。	Fundam Clin Pharmacol,2022, 10.1111/fcp.12759 J Cancer,2020, 11(4):990-996 Bioorg Med Chem,2018, 26(16):4602-4614	PC-3 cells were seeded in 6-well plates. On the next day, cells were treated with the indicated concentrations of 3-AWA, LY294002, CGP57380 or Rapamycin alone and or combination for 12 h. The cells were then subjected to preparation of whole-cell lysates for detection of the indicated proteins using western blotting. The western blots are the representative of three similar experiments.
S6888	SEL201 SEL-201 (SLV-2436, SEL201-88) 是一种高效的、ATP竞争性的 MNK1 和 MNK2 的抑制剂，对应的IC50值分别为10.8 nM和5.4 nM。
S8275	Tomivosertib (eFT-508) Tomivosertib (eFT-508) 是一种有效的、选择性的MNK1/2的抑制剂，IC50分别为2.4 nM和1 nM。它能减少肿瘤细胞的增殖和肿瘤生长。Tomivosertib (eFT-508) 可抑制 eIF4E 磷酸化并显着下调 PD-L1 蛋白质的丰度。	J Med Chem,2022, 10.1021/acs.jmedchem.1c01941 Fundam Clin Pharmacol,2022, 10.1111/fcp.12759 J Clin Invest,2021, 140752