mk2 inhibitor

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

MK2-IN-1 hydrochloride (MK 25) is a highly selective, non-ATP competitive inhibitor of p38/mitogen-activated protein kinase-activated protein kinase 2 (MAPKAPK2 or MK2, IC50: 0.11 μM) [1].

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)

MK2-IN-3 (MK2 Inhibitor III) is a potent, cell-permeable inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2 or MK-2) and can be used for the treatment of rheumatoid arthritis

Ralimetinib is a selective inhibitor that blocks phosphorylation of MK2 at Thr334, without affecting the phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc. Ralimetinib functions as an ATP-competitive inhibitor of p38 MAPK α/β, demonstrating IC50 values of 5.3 and 3.2 nM, respectively, and is under investigation as an anti-inflammatory and anticancer therapeutic.

CMPD1 is a non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor(apparent Ki (Kiapp): 330 nM).

PF-3644022 is an effective, selective, and ATP-competitive MAPKAPK2 (MK2) inhibitor (IC50: 5.2 nM and a Ki of 3 nM). PF-3644022 potently inhibits TNFα production and has an anti-inflammatory effect. PF-3644022 also inhibits MK3 and p38 regulated/activated

p38α-MK2-IN-1 (Compound 36) is an inhibitor of the p38α-MK2 complex, with an IC50 of 5 nM. This compound exhibits significant anti-inflammatory properties and has the ability to aid in joint repair.

MK2-IN-7 (Compound 144) is an inhibitor of mitogen-activated protein kinase-activated protein kinase-2 (MK2). It shows potential for research in inflammatory diseases, autoimmune disorders, and cancer.

Antitrypanosomal agent 23 is an antiparasitic compound effective against intracellular amastigotes of Trypanosoma cruzi in LLC-MK2 and C2C12 cells, demonstrating activity with IC50 values of 0.10 and 0.11 μM, respectively. It also acts as a weak inhibitor of recombinant Trypanosoma cruzi sialyltransferase (TcTS) with an IC50 of 1.1 mM.

(R)-STU104-D6 is a deuterium-labeled variant of  (R)-STU104 (T60657). This compound acts as a potent and orally active inhibitor of the interaction between TAK1 and MKK3 proteins, exhibiting IC50 values of 0.58 μM for TNF-α and 4.0 μM for MKK3 phosphorylation. By binding to MKK3, (R)-STU104 hinders TAK1's ability to phosphorylate MKK3, thereby disrupting the TAK1/MKK3/p38/MnK1/MK2/elF4E signaling pathway. It is utilized in research related to ulcerative colitis.

Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5 μM) inhibits the proliferation of KG-1a leukemia cells.3 1.Garvin, L.K., Green, N., Hu, Y., et al.Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationshipsBioor. Med. Chem. Lett.15(23)5288-5292(2005) 2.Wang, X., and Studzinski, G.P.Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cellsJ. Steroid. Biochem. Mol. Biol.121(1-2)395-398(2010) 3.Wang, X., Gocek, E., Novik, V., et al.Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3Cell Cycle9(22)4542-4551(2010)

Zunsemetinib (ATI-450) is an orally active and selective inhibitor of the p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway.Zunsemetinib is used to study spondyloarthritis and rheumatoid arthritis.

CC-99677 (Gamcemetinib) is a selectively targeted covalent MAPKAPK2 (MK2) inhibitor for autoimmune diseases that translates biochemical potency into cellular potency as demonstrated by potent inhibition of heat shock protein 27 (HSP1) phosphorylation in LPS-activated monocyte THP-27 cells via a nucleophilic aromatic substitution (SNAr) mechanism.CC-99677 in Rat experiments demonstrated potency in both biochemical (IC 50 =156.3 nM) and cellular assays (EC 50 =89 nM).

MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a potent and selective inhibitor of p38α MAPK with a Ki value of 101 nM. It exhibits excellent CNS penetration and oral bioavailability, and effectively suppresses the phosphorylation of MK2, a substrate of endogenous p38α MAPK, in activated glial cells.

MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS-penetrant, and orally active p38α MAPK inhibitor with a Ki of 101 nM. It inhibits the endogenous p38α MAPK's ability to phosphorylate the endogenous substrate MK2 in activated glia [1].

MW-150 (MW01-18-150SRM) is a unique, selective, CNS-penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.

(R)-STU104 is a novel TAK1-MKK3 protein-protein interaction (PPI) inhibitor that inhibits TNF-α and suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signalling pathway by binding to MKK3 and disrupting TAK1 phosphorylation of MKK3. (R)-STU104 is a candidate compound for the treatment of ulcerative colitis.

MK2-IN-4, a MAPKAPK2 (MK2) inhibitor with an IC50 of 45 nM, can be used in cancer, inflammation, and immunology studies.

PHA-767491 hydrochloride (CAY-10572 hydrochloride) is an effective ATP-competitive dual Cdc7/CDK9 inhibitor (IC50: 10/34 nM). It has ~20-fold selectivity against GSK3-β and CDK1/2, 50-fold selectivity against CDK5 and MK2, 100-fold selectivity against CHK2 and PLK1.

Anti-inflammatory agent 33, a potent p38α inhibitor, effectively reduces NO production and suppresses LPS-induced expression of iNOS, COX-2, p-p38α, and p-MK2 proteins, thereby demonstrating anti-inflammatory activity.

MMI-0100, a cell-permeant peptide inhibitor of mitogen-activated protein kinase activated protein kinase II (MK2), effectively reduces intimal hyperplasia ex vivo and in vivo. It specifically suppresses IL-6 expression while not affecting IL-8 expression and mitigates fibrotic processes, including vein graft disease [1].

MK2-IN-5, a pseudosubstrate of Mk2 with an inhibition constant (K_i) of 8 μM, selectively targets the protein interaction domain of the MAPK pathway and inhibits the phosphorylation of HSP25 and HSP27 [1] [2] [3].

MK2-IN-6 (Compound 11) is an effective and selective irreversible inhibitor of MK2 with an IC50 value of 2.3 nM. It suppresses the kinase activity of MK2, leading to sustained inhibition of MK2 signaling and reduction of pathological inflammatory factors in macrophages. MK2-IN-6 is capable of inhibiting the M2-like protein phenotype in macrophages both in vitro and in vivo, showing potential for use in colorectal cancer research.