MNK Inhibitor

HG-10-102-01 is a highly potent, selective, and brain-penetrable LRRK2 inhibitor, with IC₅₀ values of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. HG-10-102-01 also inhibits MNK2 and MLK1, with IC₅₀ values of 0.6 and 2.1 μM. HG-10-102-01 can be used for Parkinson's disease (PD) research.

QL-X-138 is a potent and selective BTK/MNK dual kinase inhibitor, exhibits covalent binding to BTK and non-covalent binding to MNK. QL-X-138 shows IC₅₀s of 9.4 nM, 107.4 nM and 26 nM for BTK, MNK1 and MNK2 kinases respectively. QL-X-138 also shows anti-dengue virus 2 activity, with an IC₅₀ of 3.5 μM. QL-X-138 can be used for the research of B-cell malignancies.

Cercosporamide is a highly potent, ATP-competitive PKC kinase inhibitor targeting to PKC1, with an IC₅₀ of <50 nM and a K_i of <7 nM. Cercosporamide is a unique Mnk inhibitor.

MNK-IN-5 is a MNK inhibitor that suppresses MNK activity.

ETC-501 is a blood-brain barrier-permeable, orally active, and selective MNK1/MNK2 inhibitor, with an IC₅₀ of 0.033 μM against MNK1 and 0.111 μM against MNK2. ETC-501 inhibits glioblastoma cell proliferation, impairs DNA damage repair function, delays cell cycle progression, and suppresses ribosome biogenesis. ETC-501 enhances Temozolomide (HY-17364)-induced cellular senescence, attenuates the senescence-associated secretory phenotype, and increases cellular sensitivity to Navitoclax (HY-10087). ETC-501 is applicable to research related to glioblastoma.

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-5 is a potent and selective MNK1/2 inhibitor as a therapeutic agent.

Tomivosertib hydrochlorideis a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC₅₀s of 1-2 nM against both isoforms. Tomivosertib hydrochloride treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC₅₀=2-16 nM) in tumor cell lines. Tomivosertib hydrochloride also dramatically downregulates PD-L1 protein abundance.

MNK-IN-4 (compound D25) is a potent and selective MNK inhibitor for the study of sepsis-related acute splenic injury.

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.