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.
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MAPKAPK2 (MK2) Verwandte Produkte (47)
Verwandte Produkte (47)
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Antibodies (3)
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PF-3644022
0 ImagesPF-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.
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Dehydrocostus Lactone
0 ImagesSynonyms: (-)-Dehydrocostus lactone; Epiligulyl oxideDehydrocostus Lactone ((-)-Dehydrocostus lactone) is a natural sesquiterpene that can be isolated from Saussurea lappa. Dehydrocostus Lactone has multiple activities such as anti-inflammatory, antibacterial, anti-tumor, and immunomodulatory effects. Dehydrocostus Lactone has an MIC of 2 µg/mL against Mycobacterium tuberculosis. Dehydrocostus Lactone can also inhibit the killing activity of cytotoxic T lymphocytes and induce apoptosis in tumor cells.
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Gamcemetinib
0 ImagesSynonyms: CC-99677Gamcemetinib (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.
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Kukoamine B
0 ImagesKukoamine B, a spermine alkaloid, is a potent dual LPS and CpG DNA inhibitor with Kd values of 1.23 µM and 0.66 µM, respectively. Kukoamine B exerts anti-inflammatory, anti-diabetic, anti-oxidant, anti-osteoporotic and neuroprotective effects. Kukoamine B has the potential for the study of sepsis.
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MK2-IN-3
0 ImagesMK2-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.
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HRX-0233
0 ImagesHRX-0233 is an orally potent MAP2K4 inhibitor. HRX-0233 inhibits the MAP2K4-JNK-JUN signaling pathway, blocks the feedback activation of receptor tyrosine kinases, and sustains the inhibitory effect on KRAS signaling. HRX-0233 exerts synergistic inhibition on the mTORC1 and MAPK pathways. When combined with Ipatasertib (HY-15186) or Sotorasib (HY-114277), it produces synergistic antiproliferative, pro-apoptotic (apoptosis) and antitumor effects, and shows good tolerability in mouse models. HRX-0233 can be used in CRISPR knockout screens to identify vulnerability-related genes. HRX-0233 is applicable to research related to prostate cancer, non-small cell lung cancer and colorectal cancer.
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DB1113
0 ImagesDB1113 is a multi-kinase PROTAC degrader. DB1113 induces the ubiquitination and degradation of 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 to study diseases or disorders mediated by aberrant kinase activity.
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Agrimonolide
0 ImagesAgrimonolide is a phenethyl isocoumarin compound discovered from Agrimonia pilosa, exhibiting anti-inflammatory, antioxidant, and anticancer activities. Agrimonolide inhibits NF-κB, MAPK, and TLR4-mediated neuroinflammatory signaling, suppresses Notch and JAK2/STAT3 signaling to modulate Th17/Treg balance and maintain the intestinal barrier. Agrimonolide decreases HIF1A expression, inhibits glycolysis, and induces ferroptosis and cell cycle arrest via the mTOR pathway in tumor models, thereby suppressing cancer cell viability, proliferation, and metastasis. Agrimonolide exerts hepatoprotective and anti-fibrotic effects by regulating bile acid transporter expression and reducing hepatic bile acid accumulation. Agrimonolide is used for research on ulcerative colitis, ovarian cancer, non-small cell lung cancer, cholestatic liver injury, and neuroinflammation.
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Norartocarpetin
0 ImagesNorartocarpetin 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.
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Tpl2 Kinase Inhibitor 1
0 ImagesTpl2 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.
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Proinsulin C-peptide (human)
0 ImagesProinsulin C-peptide (human) is a peptide consisting of 31 amino acids that links the A and B chains of proinsulin to ensure its correct folding. Proinsulin C-peptide (human) inhibits the high glucose-induced increase in PDGF-β receptor protein expression and the phosphorylation of p42/p44 MAP kinase. Proinsulin C-peptide (human) increases the deformability of erythrocytes derived from type 1 diabetes, inhibits insulin-induced neointimal thickening, and suppresses the proliferation of rat aortic smooth muscle cells cultured under high-glucose conditions.
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CMPD1
0 ImagesCMPD1 is a selective and non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor with apparent Ki (Kiapp) of 330 nM.
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Spinacetin
0 ImagesSpinacetin is an orally active flavonoid glycoside found in Inula japonica, with antioxidant and anti-inflammatory activities. Spinacetin inhibits major inflammatory signaling pathways such as Syk, MAPK, and NF-κB, and reduces Ca2+-dependent release of allergic mediators. Spinacetin induces protective autophagy and enhances antioxidant defense by upregulating SIRT3/SIRT1/PGC-1α, activating AMPK, and inhibiting mTOR and NF-κB, thereby exerting anti-apoptotic, cardioprotective, bladder-protective, and hepatoprotective effects. Spinacetin alleviates Doxorubicin (HY-15142A)-induced cardiotoxicity and reduces Cyclophosphamide (HY-17420)-induced hemorrhagic cystitis. Spinacetin can be used in research on allergic reactions, cardiotoxicity, cystitis, and cadmium-aggravated hepatic ischemia.
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MK2-IN-1 hydrochloride
0 ImagesMK2-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.
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MK2-IN-3 hydrate
0 ImagesMK2-IN-3 hydrate (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 8.5 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.
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C-8 Ceramide-1-phosphate
0 ImagesArt. -Nr.: HY-165099CAS. Nr.: 158983-53-0C-8 Ceramide-1-phosphate ammonium is a short-chain synthetic C1P analog that inhibits apoptosis and increases cell survival. C-8 Ceramide-1-phosphate ammonium reduces MAPK activation and cytokine expression, induces Ca2+ mobilization and ERK1/2 phosphorylation, promotes M2-like polarization, and inhibits the M1 phenotype. C-8 Ceramide-1-phosphate ammonium inhibits acidic SMase, stimulates PI3-K/PIP3 generation, and interconverts with ceramide through kinase/phosphatase activity to maintain cellular homeostasis. C-8 Ceramide-1-phosphate ammonium can be used in research related to lipid metabolism and chronic wounds.
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MK2-IN-5 acetate
0 ImagesArt. -Nr.: HY-P10072AReinheit: 99.64%Synonyms: Hsp25 kinase inhibitor acetate; Mk2 pseudosubstrate acetateMK2-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.
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MK2-IN-1
0 ImagesMK2-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.
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MMI-0100
0 ImagesSynonyms: MK2i peptide; YARA-MK2iMMI-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.
