MAPKAPK2 (MK2)

PF-3644022 is a potent and selective mitogen-activated protein kinase (MAPK)-activated protein kinase-2 (MK2) inhibitor (Ki =3 nM).

MK-2 Inhibitor III (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM.

CMPD-1 is a non-ATP-competitive, selective inhibitor of p38α-mediated MK2a (mitogen-activated protein kinase-2a) phosphorylation (apparent Ki = 330 nM).

GLPG-0259 is a small-molecule inhibitor of mitogen-activated protein kinase-activated protein kinase 5 (MAPKAPK5), a kinase enzyme that plays a role in important inflammatory pathways

MK2-IN-1 hydrochloride is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.

MMI-0100 is a cell-permeant peptide inhibitor of mitogen activated protein kinase activated protein kinase II (MK2). MMI-0100 reduces intimal hyperplasia ex vivo and in vivo. MMI-0100 suppresses IL-6 expression without effect on IL-8 expression. MMI-0100 suppresses fibrotic processes such as vein graft disease.

Norartocarpetin is a potent tyrosinase inhibitor, demonstrating significant inhibition with an IC50 value of 0.47 μM. This compound serves as an effective antibrowning agent for food systems research and exhibits notable anticancer activity against lung carcinoma cells (NCI-H460) with an IC50 of 22 μM. Its antiproliferative effects are mediated through targeting the Ras/Raf/MAPK signaling pathway, inducing mitochondrial-mediated apoptosis, causing S-phase cell cycle arrest, and inhibiting cell migration and invasion in human lung carcinoma cells.

DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions.

MK2-IN-1 is a selective inhibitor of MAPKAPK2 (MK2), exhibiting an IC50 of 0.11 µM. This compound significantly interferes with the phosphorylation of serine residues in Tfcp2l1, with an EC50 of 0.35 µM for phosphorylated HSP27. MK2-IN-1 serves as a valuable tool for studying the role of MK2 in cellular signaling pathways and its implications in various biological processes.

p38α-MK2-IN-1 is a potent inhibitor of the p38α-MK2 complex, demonstrating an IC50 of 5 nM. This compound exhibits significant anti-inflammatory properties and promotes joint repair, making it a valuable tool for studies focused on inflammation and regenerative medicine. Researchers can employ p38α-MK2-IN-1 in various applications, including drug discovery and the exploration of signaling pathways related to inflammatory responses.

MAPKAPK5-IN-1 is a specific inhibitor of MAPKAPK5, a key regulator involved in inflammatory pathways. This substituted triazolopyrazine compound demonstrates potent inhibition of MAPKAPK5 activity, making it a valuable tool for studying the molecular mechanisms underlying rheumatoid arthritis and related inflammatory conditions. Its application in research could provide insights into potential therapeutic targets for these diseases.

RMM-46 is a selective inhibitor of MAPKAPK2 (MK2), functioning as a reversible covalent modulator. It demonstrates significant biological activity in inhibiting MSK/RSK-family kinases, making it a valuable tool for research focusing on cellular signaling pathways. RMM-46 is particularly useful in studies related to cancer biology and stress response mechanisms, facilitating a deeper understanding of MK2's role in various physiological and pathological conditions.