1. Signaling Pathways
  2. MAPK/ERK Pathway
  3. MAPKAPK2 (MK2)

MAPKAPK2 (MK2)

Mitogen-activated protein kinase activated protein kinase 2; MAP kinase activated protein kinase 2; MAPK activated protein kinase 2; MAPKAP kinase 2

MAP kinase-activated protein kinase 2 (MAPKAPK2) is an enzyme that in humans is encoded by the MAPKAPK2 gene. MAPKAP kinase-2 (MK2) is originally identified by its phosphorylation of glycogen synthase at serine-7 and the corresponding serine in a peptide (GS peptide-1) modelled after the N-terminus of glycogen synthase.

MAPKAP kinase-2 is a novel protein kinase activated by mitogen-activated protein kinase. This MAP kinase activated protein kinase, termed MAPKAP kinase-2, is distinguished from S6 kinase-II (MAPKAP kinase-1) by its response to inhibitors, lack of phosphorylation of S6 peptides and amino acid sequence.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-139504
    Gamcemetinib
    Inhibitor 99.06%
    Gamcemetinib (CC-99677) is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM). Gamcemetinib is extracted from patent WO2020236636, compound 1.
    Gamcemetinib
  • HY-139553
    Zunsemetinib
    Inhibitor 99.37%
    Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases.
    Zunsemetinib
  • HY-107427
    PF-3644022
    Inhibitor 99.65%
    PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.
    PF-3644022
  • HY-12834A
    MK2-IN-1 hydrochloride
    Inhibitor 98.36%
    MK2-IN-1 hydrochloride (compound 1) is a potent and selecitve MAPKAPK2 (MK2) inhibitor with an IC50 of 0.11 uM for MK2 and an EC50 of 0.35 uM for pHSP27. MK2-IN-1 hydrochloride impaires the phosphorylation level of serine residues in the Tfcp2l1 protein.
    MK2-IN-1 hydrochloride
  • HY-12358
    Tpl2 Kinase Inhibitor 1
    Inhibitor 99.22%
    Tpl2 Kinase Inhibitor 1 is a 3-pyridylmethylamino analog, and is a selective Tpl2 inhibitor (IC50=50 nM). Tpl2 consists of COT kinase and MAP3K8. Tpl2 Kinase Inhibitor 1 plays an important role in the regulation of the inflammatory response and the progression of some cancers.
    Tpl2 Kinase Inhibitor 1
  • HY-159190
    HRX-0233
    Inhibitor
    HRX-0233 is a small-molecule MAP2K4 inhibitor. HRX-0233 results in strong tumor shrinkage without any apparent toxicity in H358 KRASG12C-mutant non-small cell lung cancers (NSCLC) in vivo. HRX-0233 efficiently prevents feedback activation of receptor tyrosine kinases (RTKs) upon monotherapy KRAS inhibitor Sotorasib (HY-114277) and causes a more sustained and complete inhibition of MAPK signaling. HRX-0233 is promising for research of AR-negative prostate cancer, lung and colon cancers.
    HRX-0233
  • HY-P10367
    Ziptide
    Ziptide is a substrate for MAPK activated protein kinase 2 (MAPKAPK2, Km = 5 μM), MAPKAPK3 (Km = 30 μM), PARK (Km = 40 μM), checkpoint kinase 1 (Chk1, Km = 5 μM), AMP-activated protein kinase (AMPK, Km = 75 μM), and calcium/calmodulin-dependent protein kinase II (CamKII, Km = 300 μM).
    Ziptide
  • HY-131249
    MK2-IN-3
    Inhibitor 99.58%
    MK2-IN-3 is a potent and selective inhibitor of MAPKAP-K2 (MK-2), with an IC50 of 8.5 nM. MK2-IN-3 shows selectivity for MK-2 over MK-3, MK-5, ERK2, MNK1, p38a (IC50s=0.21, 0.081, 3.44, 5.7, and >100 μM, respectively) and MSK1, MSK2, CDK2, JNK2, IKK2 (IC50s>200 μM). MK2-IN-3 can reduce TNFα production in both U937 cells and in vivo.
    MK2-IN-3
  • HY-N10503
    Norartocarpetin
    98.92%
    Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells.
    Norartocarpetin
  • HY-108643
    CMPD1
    Inhibitor 99.86%
    CMPD1 is a selective and non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor with apparent Ki (Kiapp) of 330?nM.
    CMPD1
  • HY-P3412
    MMI-0100
    98.83%
    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.
    MMI-0100
  • HY-P10072A
    MK2-IN-5 acetate
    98.46%
    MK2-IN-5 (Hsp25 kinase inhibitor) acetate is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 acetate targets the protein interaction domain in the MAPK pathway. MK2-IN-5 acetate inhibits HSP25 and HSP27 phosphorylation.
    MK2-IN-5 acetate
  • HY-112457
    MK2-IN-3 hydrate
    Inhibitor ≥99.0%
    MK2-IN-3 hydrate (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM.MK2-IN-3 hydrate is exceptional selectivity against MK-3 (IC50=0.21 μM), MK-5 (IC50=0.081 μM), ERK2 (IC50=3.44 μM), MNK1(IC50=5.7 μM) as well as CDK2, JNK2, IKK2, MSK1, and MSK2.
    MK2-IN-3 hydrate
  • HY-148061
    DB1113
    99.28%
    DB1113 (Example 24) is a bifunctional compound targeted protein degradation of kinases. DB1113 degrades ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. DB1113 can be used for research of disease or disorder mediated by aberrant kinase activity.
    DB1113
  • HY-157793
    SMU-L11
    Activator 99.64%
    SMU-L11 is a specific TLR7 agonist (EC50=0.024 μM), which recruits MyD88 adapter protein and activates downstream NF-κB and MAPK signaling pathways. In murine models, SMU-L11 significantly enhances immune cell activation and promotes the proliferation of CD4+ T and CD8+ T cells, thereby directly killing tumor cells and inhibiting tumor growth. SMU-L11 can be used for cancer research, and also has the potential for studying immune system diseases.
    SMU-L11
  • HY-12834
    MK2-IN-1
    Inhibitor
    MK2-IN-1 (compound 1) is a potent and selecitve MAPKAPK2 (MK2) inhibitor with an IC50 of 0.11 uM for MK2 and an EC50 of 0.35 uM for pHSP27. MK2-IN-1 impaires the phosphorylation level of serine residues in the Tfcp2l1 protein.
    MK2-IN-1
  • HY-147283
    MK2-IN-4
    Inhibitor
    MK2-IN-4 is a MAPKAPK2 (MK2) inhibitor with an IC50 value of 45 nM. MK2-IN-4 can be used in the research of cancer, inflammation, immunology.
    MK2-IN-4
  • HY-W726640
    Peraquinsin
    Activator
    Peraquinsin is a MK2 activator. Peraquinsin can be used for the research of vascular disorder or endothelial barrier disorder. Peraquinsin also is an antihypertensive agent.
    Peraquinsin
  • HY-106477
    Quazinone
    Inhibitor
    Quazinone is a selective inhibitor of cGMP-inhibited-phosphodiesterase (cGI-PDE, PDE3). Quazinone inhibits the phosphorylation of p42/p44 MAP kinase. Quazinone possesses antimitogenic effect .
    Quazinone
  • HY-116533
    RMM-46
    Inhibitor
    RMM-46 is a selective and reversible covalent inhibitor for MSK/RSK-family kinases.
    RMM-46
Cat. No. Product Name / Synonyms Application Reactivity