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THP-1 macrophages

" in MedChemExpress (MCE) Product Catalog:

20

Inhibitors & Agonists

1

Peptides

2

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-151132

    IsoQC-IN-1

    CD47 Cancer
    Glutaminyl cyclases-IN-1 (IsoQC-IN-1) is a potent glutaminyl cyclases (QC) inhibitor with IC50 values of 12 nM and 73 nM for human QC and isoQC, respectively. Glutaminyl cyclases-IN-1 can selectively interfere with the interaction of CD47/SIRPα through isoQC inhibition, and enhances the increased phagocytic activity of both THP-1 and U937 macrophages .
    Glutaminyl cyclases-IN-1
  • HY-123942
    Diprovocim
    Maximum Cited Publications
    9 Publications Verification

    Toll-like Receptor (TLR) TNF Receptor p38 MAPK NF-κB Inflammation/Immunology Cancer
    Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses .
    Diprovocim
  • HY-147017

    GSK286

    Bacterial Infection Inflammation/Immunology
    GSK2556286 (GSK286) is an orally active and cholesterol-dependent Mycobacterium tuberculosis inhibitor. GSK2556286 inhibits Mycobacterium tuberculosis inside infected macrophages (IC50 = 0.07 μM in THP-1 cells), in the presence of cholesterol. GSK2556286 acts via Rv1625c, a membrane-bound adenylyl cyclase in Mycobacterium tuberculosis. GSK2556286 is an Rv1625 agonist leading to increased cAMP and reduced cholesterol metabolism. GSK2556286 can be studied in research for antitubercular purposes .
    GSK2556286
  • HY-144226
    NLRP3/AIM2-IN-3
    5+ Cited Publications

    NOD-like Receptor (NLR) AIM2 Pyroptosis Inflammation/Immunology
    NLRP3/AIM2-IN-3 (compound 59) is a potent inhibitor with differential species specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis. NLRP3/AIM2-IN-3 shows inhibitory efficacy against pyroptosis in THP-1 macrophages stimulated with LPS/nigericin, with an IC50 of 0.077 ± 0.008 μM. NLRP3/AIM2-IN-3 disturbs the interaction of NLRP3 or AIM2 with the adaptor protein ASC and inhibited ASC oligomerization .
    NLRP3/AIM2-IN-3
  • HY-168089

    NOD-like Receptor (NLR) Inflammation/Immunology
    NLRP3-IN-49 (compound Z48) is a potent and specific NLRP3 inhibitor (IC50=0.26 μM in THP-1 cells, IC50=0.21 μM in mouse bone marrow macrophages). NLRP3-IN-49 can directly bind to NLRP3 protein (Kd=1.05 μM), effectively preventing the assembly and activation of NLRP3 inflammasome, thereby exhibiting anti-inflammatory properties. NLRP3-IN-49 can be used in the study of inflammatory bowel disease .
    NLRP3-IN-49
  • HY-168520

    NOD-like Receptor (NLR) Inflammation/Immunology
    NLRP3-IN-57 (compound 5) inhibits the NLRP3 inflammasome, thereby reducing IL-1β levels in LPS plus Nigericin-induced THP-1 macrophages. .
    NLRP3-IN-57
  • HY-174144

    Prostaglandin Receptor Inflammation/Immunology
    RJG-2036 is a potent covalent inhibitor of human prostaglandin reductase 2 (PTGR2)(IC50=100 nM). RJG-2036 inhibits NADPH-dependent reduction, significantly reducing secretion of proinflammatory cytokines like TNF-α and multiple eicosanoids in LPS-stimulated THP-1 macrophages. RJG-2036 is promising for research of inflammatory diseases .
    RJG-2036
  • HY-162122

    PPAR Inflammation/Immunology
    PPARα/γ agonist 3 (Compound 4) is a dual agonist of PPARα/γ. PPARα/γ agonist 3 has anti-inflammatory activity, significantly reducing inflammatory markers such as IL-6 and MCP-1 on THP-1 macrophages through NF-κB activation. PPARα/γ agonist 3 can be used in the study of metabolic syndrome and metabolic dysfunction-related fatty liver disease (MAFLD) .
    PPARα/γ agonist 3
  • HY-131040

    NOD-like Receptor (NLR) Inflammation/Immunology
    NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor (IC50= 574 nM) that acts independently of Ca 2+. NLRP3-IN-NBC6 inhibits Nigericin (HY-127019)-induced inflammasome activation in THP-1 cells and Imiquimod (HY-B0180)-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs) .
    NLRP3-IN-NBC6
  • HY-N3887

    Haplophytin B; Haplophytine B

    Bacterial Infection
    Evoxine (Haplophytin B) is a compound that selectively inhibits CO2-induced immunosuppression and has activity in inhibiting the expression of interleukin-6 and chemokine CCL2 in human THP-1 macrophages. Evoxine shows antimicrobial activity against a wide range of bacteria, especially performing well in minimum inhibitory concentration (MIC) tests against Escherichia coli, Bacillus subtilis, and Staphylococcus aureus. Evoxine extracts may find application in crude drug preparations in West Africa, provided that their in vivo toxicity results are negative .
    Evoxine
  • HY-100401A

    CS-505

    Acyltransferase Cardiovascular Disease
    Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively . Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity .
    Pactimibe sulfate
  • HY-100401

    CS-505 free base

    Acyltransferase Cardiovascular Disease
    Pactimibe (CS-505 free base) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively . Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity .
    Pactimibe
  • HY-176256

    STING Cancer
    endo-S-cGAFMP (Compound 3) is a STING agonist. endo-S-cGAFMP induces the production of interferon regulatory factors and proinflammatory cytokines by activating the cGAS-STING pathway, thereby enhancing innate and adaptive immune responses. endo-S-cGAFMP has potent immunostimulatory capacity in THP1 monocytes and RAW macrophages (EC50 values of 2.45 μM and 5.54 μM, respectively). endo-S-cGAFMP has significant antitumor activity. endo-S-cGAFMP can be used as a potential cancer immunotherapeutic agent, especially for studies of systemic administration .
    endo-S-cGAFMP
  • HY-163782

    Autophagy Phosphatase Infection
    SMIP-031 is a potent and orally active PPM1A inhibitor with an IC50 value of 180 nM. SMIP-031 induces autophagy. SMIP-031 inhibits Mycobacterium tuberculosis infect in mice .
    SMIP-031
  • HY-P10972

    Glucose-dependent Insulinotropic Peptide (22-51) (human)

    NF-κB MMP Calcium Channel Cardiovascular Disease Neurological Disease
    GIP (22-51) human (Glucose-dependent Insulinotropic Peptide (22-51) human) is a potent proatherosclerotic peptide hormone consisting of 30 amino acids. GIP (22-51) human can activate the NF-κB signaling pathway, promote the expression of MMP-8, and induce the expression of proinflammatory and proatherosclerotic proteins. GIP (22-51) human can also increase the level of intracellular free Ca 2+ in THP-1-induced macrophages. GIP (22-51) human can be used in the research of atherosclerosis .
    GIP (22-51) human
  • HY-149493

    PI3K Inflammation/Immunology Cancer
    IHMT-PI3K-455 (Compound 15u) is a potent, selective, orally active PI3Kγ/δ dual inhibitor with IC50s of 7.1 nM and 0.57 nM for PI3Kγ and PI3Kδ, respectively. IHMT-PI3K-455 suppresses the AKT phosphorylation. IHMT-PI3K-455 inhibits tumor growth by recruiting and activating more CD8 + killing T cells.IHMT-PI3K-455 is used in cancer research .
    IHMT-PI3K-455
  • HY-Y0366
    Lauric acid
    3 Publications Verification

    Endogenous Metabolite Bacterial Infection
    Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively .
    Lauric acid
  • HY-18620
    DZ2002
    1 Publications Verification

    STAT PI3K NF-κB MEK ERK Bacterial Antibiotic Akt Inflammation/Immunology
    DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis .
    DZ2002
  • HY-18620R

    STAT PI3K NF-κB MEK ERK Bacterial Antibiotic Akt Inflammation/Immunology
    DZ2002 (Standard) is the analytical standard of DZ2002. This product is intended for research and analytical applications. DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis .
    DZ2002 (Standard)
  • HY-163032

    FABP Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    FABP4-IN-3 (compound C3) is a highly selective FABP4 inhibitor (FABP4 Ki = 25 ± 3 a nM, FABP3 Ki = 15.03 μM) which exhibits a 601-fold selectivity over FABP3. FABP4-IN-3 also shows metabolic stability and potent cellular anti-inflammatory activity, making it promising to get involved in the research of metabolic disease, cardiac dysfunction and inflammation-related disease .
    FABP4-IN-3

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