MAPKAPK2 (MK2) Inhibitor
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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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INHIB1X
0 ImagesCat. No.: HY-182596CAS No.: 1105659-16-2INHIB1X is a tetracyclic MAPKAP-K2 (MK2) inhibitor with an IC50 of 0.02 μM. INHIB1X inhibits LPS-induced TNFα release in human peripheral blood mononuclear cells (hPBMCs). INHIB1X suppresses the phosphorylation of hsp27 in Anisomycin-stimulated THP-1 cells. INHIB1X can be used for the research of inflammatory and tumor diseases.
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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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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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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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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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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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CBP-501
0 ImagesCat. No.: HY-16129CAS No.: 565434-85-7CBP-501, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 is used for various types of cancer.
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SHP2-IN-33
0 ImagesCat. No.: HY-168715CAS No.: 2894017-46-8SHP2-IN-33 (Compound D13) is an allosteric inhibitor of SHP2 with an IC50 of 1.2 μM. In cellular studies, SHP2-IN-33 demonstrates antiproliferative activity with an IC50 of 38 μM against Huh7 cells by arresting the G0/G1 cell cycle, promoting apoptosis (Apoptosis), and suppressing the MAPK signaling pathway. In an in vivo Huh7 xenograft mouse model, SHP2-IN-33 exhibits significant antitumor activity and favorable pharmacokinetics, including 54% oral bioavailability and a half-life of 10.57 hours. SHP2-IN-33 is a promising compound for studying tumor diseases associated with SHP2.
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MK2-IN-7
0 ImagesCat. No.: HY-169513CAS No.: 77607-70-6MK2-IN-7 (Compound 144) is a mitogen activated protein kinase-activated protein kinase-2 (MK2) inhibitor. MK2-IN-7 is promising for research of inflammatory diseases, autoimmune diseases and cancer.
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MK2-IN-4
0 ImagesCat. No.: HY-147283CAS No.: 1105658-32-9MK2-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.
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