DS12881479 is a potent and selective Mnk1 inhibitor with an IC50 value of 21 nM. DS12881479 can be used in cancer research[1].
QL-X-138 is a selective and potent BTK/MNK dual kinase inhibitor with IC50 of 8, 107.4, and 26 nM for BTK, MNK1, and MNK2, respectively; exhibits covalent binding to BTK and noncovalent binding to MNK; enhances the antiproliferative efficacies in vitro against a variety of B-cell cancer cell lines, as well as AML and CLL primary patient cells; arrests cell cycle progression and strongly induces apoptosis.
EB1 is the inhibitor of kinases MNK with IC50s of 0.69 μM (MNK1) and 9.4 μM (MNK2). EB1 selectively inhibits the growth of cancer cells, but not normal cells. EB1 also increases cell apoptosis and suppresses eIF4E phosphorylation[1][2].
ETC-206 is a selective MNK1 and MNK2 inhibitor with IC50s of 64 nM and 86 nM, respectively.
eFT508 is a potent, highly selective, and orally bioavailable MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms.
MNK1/2-IN-5 is a potent and selective MNK1/2 inhibitor as a therapeutic agent.
CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC50 of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.
SLV-2436 is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50s of 10.8 nM and 5.4 nM, respectively.
MNK inhibitor 9 is a potent, selective MAPK-interacting kinase (MNK1 and MNK2) inhibitor with IC50 of 3 nM for both, with no activity aginst CDK1/2 (IC50>25 uM); displays excellent selectivity against a 53 kinase panel, with 4 kinases with IC50 <1 uM; inhibits eIF4E phosphorylation in KMS11-luc myeloma with IC50 of 0.6 nM, exhibits inhibition of cell proliferation in human multiple myeloma tumor cell line with EC50 of 1.7 uM; has good solubility and permeability, and is a suitable in vivo tool compound.
Cercosporamide is a highly potent, ATP-competitive Pkc1 kinase inhibitor, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor.