MNK Inhibitor

HSND80 (Compound 1) is an orally active inhibitor of MNK/p70S6K, with K_d values of 44 nM against MNK1 and 4 nM against MNK2. HSND80 has a longer target residence time of 45 mins and 58 mins against MNK1 and MNK2 respectively. HSND80 can suppress non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppress Triple-Negative Breast Cancer (TNBC) in vitro.

MNK1/2-IN-6 is a potent and selective MNK1/2 inhibitor with IC₅₀s of 2.3 nM and 3.4 nM for MNK1 and MNK2, respectively. MNK1/2-IN-6 induces apoptosis in a concentration-dependent manner.

MNK1/2-IN-10 is an orally active, selective MNK1/MNK2 inhibitor, with an IC₅₀ of 10.84 nM for MNK1 and an IC₅₀ of 12.81 nM for MNK2. MNK1/2-IN-10 inhibits eIF4E phosphorylation, the NF-κB signaling pathway, macrophage polarization, oxidative stress and the production of pro-inflammatory cytokines. MNK1/2-IN-10 alleviates kidney and spleen damage in LPS (HY-D1056)-induced inflammatory mouse models. Anti-inflammatory agent 115 is applicable for research related to acute inflammation.

MNK1/2-IN-11 is a potent, selective and orally active MNK1/2 inhibitor with MNK1 IC₅₀ of 1.2 nM, MNK2 IC₅₀ of 1.3 nM. MNK1/2-IN-11 reduces eukaryotic translation initiation factor 4E phosphorylation, decreases Mcl-1 and Cyclin D1 expression. MNK1/2-IN-11 inhibits tumor growth in mouse CT26 colorectal tumor models. MNK1/2-IN-11 can be used for the research of colorectal cancer.

K783-0308 is a potent and selective dual inhibitor of FLT3 and MNK2 with IC₅₀ values of 680 and 406 nM, respectively. K783-0308 inhibits the growth of MOLM-13 (IC₅₀=10.5 µM) and MV-4-11 (IC₅₀=10.4 µM) cells. K783-0308 promotes acute myeloid leukemia (AML) cell apoptosis and cell cycle arrests in the G0/G1 phase.

YTB53 is a MNK1 and MNK2 inhibitor with IC₅₀s of 37 nM and 9 nM, respectively. YTB53 inhibits PDGFRα, TRKB and FLT3 in leukemia cells. YTB53 induces cell cycle arrest, apoptosis, pyroptosis, and mitochondrial dysfunction. YTB53 exhibits antiangiogenic effects. YTB53 can be used for the study of acute myeloid leukemia (AML).

MNK1/2-IN-8 (compound 15b) is a MNK1/2 inhibitor with the IC₅₀ values of 0.8 and 1.5 nM against Mnk1 and Mnk2. MNK1/2-IN-8 shows anti-proliferative activity and induces cell cycle arrest.

Multi-kinase-IN-12 is a non-selective multi-target inhibitor, with IC₅₀ values against human targets as follows: Flt3 < 0.001 μM, c-Src 0.002 μM, KDR 0.004 μM, Eph-A2, MNK-1 and Flt1 0.011 μM, Lck 0.016 μM, Rsk1 0.21 μM, and α2 subunit of AMPK 0.041 μM. Multi-kinase-IN-12 can be used in research related to solid tumors.

MNK1/2-IN-7 (compound 20j) is an orally available inhibitor of MNK1/2 with anticancer activity and hERG safety. MNK1/2-IN-7 also inhibits the phosphorylation of eIF4E, inhibiting the MNK/eIF4E signaling pathway and cancer cell proliferation. MNK1/2-IN-7 is synergistic with Ibrutinib (HY-109970).

NUCC-0231068 is a MNK1 and MNK2 inhibitor with IC₅₀ values of 8 nM and 7 nM, respectively. NUCC-0231068 inhibits the phosphorylation of eukaryotic translation initiation factor 4E (eIF4E) at Ser209, with an IC₅₀ of 23 nM in its purified form and 17 nM in its D2B form. NUCC-0231068 can be used in studies related to glioblastoma.

CGP 57380 (Standard) is the analytical standard of CGP 57380 (HY-10520). This product is intended for research and analytical applications. 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.

MNK-IN-6 (compound 1) is an inhibitor of MNK that can be used in the research of neuropathic pain.

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