CGP 57380抑制剂、激动剂(CAS号522629-08-9)CGP 57380是可渗透入细胞的Mnk1抑制剂,IC50为2.2 μM,对p38,JNK1,ERK1/2,PKC和Src样激酶无抑制性。 CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 (IC50 = 2.2 μM) with no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.
IC50 value: 2.2 uM
Target: Mnk1
in vitro: Inhibition of MNK1 activity by a specific inhibitor (CGP57380) enhanced differentiation of HL60 and 32D cells, further suggesting a role for MNK1 in the myeloid differentiation. CGP 57380 effectively inhibits eIF4E phosphorylation (IC50 = 3 μM) by MNK1 in 293 human embryonic kidney cells and serves as a useful tool in studying Mnk1-mediated cellular signaling. CGP 57380 is an inhibitor of ARK-2, BRSK2, ChoK, Dyrk3, Lck, Mnk2 and SGK.