mnk

QL-X-138 is a potent and selective BTK and MNK dual kinase inhibitor that binds covalently to BTK and non-covalently to MNK. The IC50 values of QL-X-138 are 9.4 nM for BTK, 107.4 nM for MNK1, 26 nM for MNK2, and 3.5 μM against Dengue 2. QL-X-138 is used in the study of B-cell malignancies and B-cell malignant tumors.

SLV-2436 (SEL201-88) is a novel effective and ATP-competitive inhibitor of MNK1 and MNK2 (IC50: 10.8/5.4 nM).

MNK/PIM-IN-1 is a novel dual inhibitor targeting both MNK and PIM pathways, characterized by its favorable pharmacokinetic profile.

MNK Inhibitor 9 is a potent, selective inhibitor of MNK1 2, demonstrating IC50 values of 0.003 µM for both MNK1 and MNK2. It exhibits good cell permeability, making it suitable for tumor-related research.

ROTACMNK1degrader-1 is a selective MNK1 PROTAC degrader with a DC50 of 11.92 nM and a Dmax greater than 96% in MV4-11 cells. It significantly reduces p-eIF4E levels with an IC50 of 22.07 nM, induces apoptosis, and causes cell cycle arrest at the G1 phase. This compound exhibits potent antitumor activity, demonstrating strong anti-leukemic effects in MV4-11 xenograft mouse models with acceptable drug safety.

MNK1 2-IN-5 is a potent and selective MNK1 2 inhibitor with anticancer activity and can be used to study solid tumors and hematological malignancies.

MNK1 2-IN-7 (compound 20j) serves as an orally administered inhibitor targeting MNK1 2, known for its anticancer properties and hERG safety. It also blocks the phosphorylation of eIF4E, thereby disrupting the MNK eIF4E signaling pathway and reducing cancer cell growth. Additionally, MNK1 2-IN-7 synergizes effectively with Ibrutinib. [15] [1]

MNK8 (3-methyl-6-(naphthalen-1-yl)pyrimidine-2,4(1H,3H)-dione) is a potent STAT3 inhibitor that reduces the ability of STAT3 to bind to DNA and also has a good growth inhibition effect on liver cancer cells [1].

MNK1 2-IN-6 is a potent and selective inhibitor of MNK1 (IC50: 2.3 nM) and MNK2 (IC50: 3.4 nM) that induces apoptosis in a concentration-dependent manner.

MNK1 2-IN-8 (compound 15b) serves as an inhibitor of MNK1 2, exhibiting potent IC 50 values of 0.8 nM for Mnk1 and 1.5 nM for Mnk2. Additionally, this compound demonstrates anti-proliferative effects and induces cell cycle arrest.

AZ7550, an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).

HSN748 is an analog of ponatinib and acts as a multi-kinase inhibitor. It exhibits inhibitory activity against kinases such as FLT3, ABL1, RET, PDGFRα β, MNK1, and MNK2. HSN748 can suppress the growth of chronic myeloid leukemia and acute myeloid leukemia cell lines, making it a useful compound in leukemia research.

NUCC-0200808 (Compound 12g) is an MNK1 inhibitor with an IC50 of 42 nM. It reduces eIF4E phosphorylation and cell viability in AML cells and induces apoptosis. NUCC-0200808 shows potential for research in the field of leukemia.

DS12881479 can be used in cancer research which is a potent and selective inhibitor of Mnk1(IC 50 =21 nM) [1].

QL-X-138 HCl is a novel selective and highly potent BTK MNK dual-kinase inhibitor with anticancer activity that binds covalently to BTK and noncovalently to MNK. QL-X-138 HCl inhibited BTK, MNK1, and MNK2 kinases. QL-X-138 HCl has anti-dengue virus 2 activity and shows anti-proliferative activity in acute myeloid leukemia cells. QL-X-138 HCl can be used to study lymphoma and leukemia.

Tomivosertib (eFT508) is a potent and highly selective MNK1 and MNK2 inhibitor with an IC50 value of 1-2 nM.

ETC-206 is a selective inhibitor of MNK1 and MNK2 (IC50s: 64 nM and 86 nM).

HSND80 (Compound 1) is an orally active MNK/p70S6K inhibitor, exhibiting a Kd value of 44 nM for MNK1 and 4 nM for MNK2. The residence time of HSND80 on MNK1 and MNK2 is 45 minutes and 58 minutes, respectively. HSND80 effectively inhibits non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppresses the growth of triple-negative breast cancer (TNBC) cells in vitro.

CGP 57380 (MNK1 Inhibitor) is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases.

EB1 is a potent and selective MNK kinase inhibitor with inhibitory effects on MNK1 and MNK2 with IC50 values of 0.69 μM and 9.4 μM, respectively.EB1 inhibits the growth of cancer cells, promotes apoptosis, and inhibits the phosphorylation of eIF4E.

MK2-IN-3 hydrate (MK-2 Inhibitor III) is an orally active, selective, and ATP-competitive inhibitor of MAPKAP-K2 (MK-2) (IC50 of 0.85 nM)

Cercosporamide is a ATP-competitive Pkc1 kinase inhibitor (IC50 <50 nM; Ki <7 nM). It also is a unique Mnk inhibitor.

HG-10-102-01 is an inhibitor of leucine-rich repeat kinase 2 (LRRK2, IC50 of 20.3 nM).

ETC-168 is a selective, orally active MNK inhibitor with IC50 values of 23 nM for MNK1 and 43 nM for MNK2. It demonstrates antiproliferative efficacy both in vivo and in vitro [1].