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THP-1 cells

" in MedChemExpress (MCE) Product Catalog:

129

Inhibitors & Agonists

3

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12

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18739
    Phorbol 12-myristate 13-acetate
    Maximum Cited Publications
    480 Publications Verification

    PMA; Phorbol myristate acetate

    		 PKC SphK NF-κB Inflammation/Immunology
    Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator . Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells (Validated by MedChemExpress (MCE)) .
    Phorbol 12-myristate 13-acetate
  • HY-108670
    AZ 11645373

    		P2X Receptor Inflammation/Immunology
    AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors，AZ11645373 inhibits ATP-evoked IL-1β release from lipopolysaccharide-activated THP-1 cells , with an IC50 value of 90 nM .
    AZ 11645373
  • HY-122941
    Viscidulin II

    		Interleukin Related Inflammation/Immunology
    Viscidulin II (FL6) is a flavone. Viscidulin II can be isolated from the root of Scutellaria baicalensis. Viscidulin II significantly suppresses P. acnes-induced IL-8 and IL-1β production in THP-1 cells .
    Viscidulin II
  • HY-147506
    NOD2 antagonist 1

    		NOD-like Receptor (NLR) Inflammation/Immunology
    NOD2 antagonist 1 (compound 32) is a potent and selective NOD2 antagonist with an IC50 of 5.23 μM. NOD2 antagonist 1 inhibits Muramyl dipeptide (MDP)-induced IL-8 secretion in THP-1 cells and inhibits MDP-induced IL-6, IL-10, TNF-α release in PBMCs .
    NOD2 antagonist 1
  • HY-123270
    RP23618

    		CCR Infection Inflammation/Immunology
    RP23618 is a non peptidic RANTES antagonist with the IC50 of 3 μM. RP23618 inhibit RANTES-induced chemotaxis of THP-1 cells .
    RP23618
  • HY-18739R
    Phorbol 12-myristate 13-acetate (Standard)

    		PKC SphK NF-κB Inflammation/Immunology
    Phorbol 12-myristate 13-acetate (Standard) is the analytical standard of Phorbol 12-myristate 13-acetate. This product is intended for research and analytical applications. Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator . Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells (Validated by MedChemExpress (MCE)) .
    Phorbol 12-myristate 13-acetate (Standard)
  • HY-146581
    Cathepsin C-IN-4

    		Cathepsin Inflammation/Immunology
    Cathepsin C-IN-4 (compound SF27) is a potent Cathepsin C (Cat C) inhibitor, with an IC50 of 65.6 nM. Cathepsin C-IN-4 also inhibits THP-1 and U937 cell, with IC50 values of 203.4 and 177.6 nM, respectively .
    Cathepsin C-IN-4
  • HY-146580
    Cathepsin C-IN-3

    		Cathepsin Inflammation/Immunology
    Cathepsin C-IN-3 (compound SF11) is a potent Cathepsin C (Cat C) inhibitor, with an IC50 of 61.79 nM. Cathepsin C-IN-3 also inhibits THP-1 and U937 cell, with IC50 values of 101.5 and 86.5 nM, respectively .
    Cathepsin C-IN-3
  • HY-129340
    AS-183

    		Acyltransferase Cardiovascular Disease
    AS-183 is an inhibitor of cholesterol acyltransferase (ACAT) (IC50=0.94 µM). AS-183 also inhibits the formation of cholesterol esters in HepG2, CaCo2 and THP-1 cells with IC50 values ​​of 18.1, 25.5 and 34.5 µM, respectively. AS-183 can be used in the study of atherosclerosis and hypercholesterolemia .
    AS-183
  • HY-146283
    LSD1-IN-18

    		Histone Demethylase Cancer
    LSD1-IN-18 (compound 7) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.156 μM and KD of 0.075 μM, respectively. LSD1-IN-18 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.16 and 0.21 μM, respectively .
    LSD1-IN-18
  • HY-146284
    LSD1-IN-19

    		Histone Demethylase Cancer
    LSD1-IN-19 (compound 29) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.108 μM and KD of 0.068 μM, respectively. LSD1-IN-19 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.17 and 0.40 μM, respectively .
    LSD1-IN-19
  • HY-172873
    HDSI-18

    		HDAC Caspase Apoptosis Cancer
    HDSI-18 is an orally active HDAC6 selective inhibitor (IC50: 1.6 nM). HDSI-18 is cytotoxic to K562, MV4-11, MOLM-13, THP-1, and Jurkat cells (IC50: 0.48, 0.58, 0.91, 1.79, and 4.31 μM, respectively). HDSI-18 activates Caspase-3, induces mitochondrial depolarization and apoptosis, and has antitumor activity .
    HDSI-18
  • HY-173422
    MS2133

    		PROTACs Histone Methyltransferase Cancer
    MS2133 is a DOT1L PROTAC degrader. MS2133 promotes ubiquitination and degradation of DOT1L in THP-1 and MV4-11 cells (DC50: 56 nM and 25 nM, respectively), and reduces H3K79 methylation. MS2133 inhibits the growth of MLL-r leukemia cells and has anticancer activity. (Pink: DOT1L ligand (HY-173423); Blue: E3 ligase VHL ligand (HY-47070); Black: Linker (HY-79577); E3 ligase VHL ligand-linker conjugate (HY-173424)) .
    MS2133
  • HY-153673
    PROTAC IRAK4 degrader-8

    		IRAK PROTACs Cancer
    PROTAC IRAK4 degrader-8 (Compound 2) is a PROTAC IRAK4 degrader (IC50: 15.5 nM). PROTAC IRAK4 degrader-8 degrades IRAK4 in THP-1 cells (DC50: 1.8 nM)。PROTAC IRAK4 degrader-8 also inhibits L-6 production in human whole blood and LPS-induced human PBMC cells, with IC50s of 246 nM and 2.2 nM respectively .
    PROTAC IRAK4 degrader-8
  • HY-146285
    LSD1-IN-20

    		Histone Demethylase Histone Methyltransferase Cancer
    LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively .
    LSD1-IN-20
  • HY-171589
    NLRP3-IN-77

    		NOD-like Receptor (NLR) Interleukin Related Inflammation/Immunology Cancer
    NLRP3-IN-77 (Compound 7n) is a potent NLRP3 inflammasome inhibitor. NLRP3-IN-77 inhibits the viability of THP-1 cells with an IC50 value of 5.36 nM. NLRP3-IN-77 can effectively reduce the secretion of interleukin-1β (IL-1β) and interleukin-18 (IL-18). NLRP3-IN-77 is promising for research of diseases related to the abnormal activation of the NLRP3 inflammasome, such as cancer and inflammatory diseases .
    NLRP3-IN-77
  • HY-134375
    cAIMP

    Cyclic Adenosine-Inosine Monophosphate

    		 NF-κB IFNAR Inflammation/Immunology
    cAIMP (Cyclic Adenosine-Inosine Monophosphate) is an effective synthetic cyclic dinucleotide. cAIMP activates IRF and NF-κB in the THP1 human monocyte reporter cell line (THP1-Dual). cAIMP induces the secretion of IFNs and pro-inflammatory cytokines in vitro in human blood, with an EC50 of 6.4 μmol/L .
    cAIMP
  • HY-104073
    CAY10602
    5+ Cited Publications

    		 Sirtuin Metabolic Disease Inflammation/Immunology
    CAY10602 is a SIRT1 activator. CAY10602 dose-dependently suppresses the NF-κB-dependent induction of TNF-α by lipopolysaccharide in THP-1 cells .
    CAY10602
  • HY-N12469
    Gypsogenin 3-O-glucuronide

    		Others Others
    Gypsogenin 3-O-glucuronide is a glucuronide that can be isolated from Gypsophila. Gypsogenin 3-O-glucuronide has cytotoxic effect on THP-1 cells .
    Gypsogenin 3-O-glucuronide
  • HY-144168A
    STING agonist-8 dihydrochloride

    		STING Inflammation/Immunology
    STING agonist-8 dihydrochloride (compound 5-AB) is a potent STING agonist with an EC50 of 27 nM in THP1-Dual KI-hSTING-R232 cells .
    STING agonist-8 dihydrochloride
  • HY-N8390
    3-Epidehydropachymic acid

    		Others Cancer
    3-Epidehydropachymic acid, a lanostane triterpenoid, shows totoxicity effect against human acute monocytic leukemia cell line THP-1 (IC50=52.51 μM) .
    3-Epidehydropachymic acid
  • HY-132221
    CU-32

    		Cyclic GMP-AMP Synthase Inflammation/Immunology
    CU-32 is a potent cGAS inhibitor with an IC50 of 0.45 µM. CU-32 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells .
    CU-32
  • HY-175003
    HV1-IN-2

    		Others Cancer
    HV1-IN-2 (Compound 14c) is a human voltage-gated proton channel (HV1) inhibitor with an IC50 of 2.14 μM. HV1-IN-2 has a potent anticancer activity with significant antiproliferative effects against THP-1 and MCF-7 cells. HV1-IN-2 can be used for cancers research, such as colorectal tumours, leukaemia, and breast cancer .
    HV1-IN-2
  • HY-N12186
    Sibiricine

    		Others Inflammation/Immunology
    Sibiricine (Compound 8) is an isoquinoline alkaloid derived from the medicinal plant Corydalis crispa. Sibiricine has significant anti-inflammatory activity on TNF-α production by LPS-activated THP-1 cells .
    Sibiricine
  • HY-168089
    NLRP3-IN-49

    		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-144168
    STING agonist-8

    		STING Inflammation/Immunology
    STING agonist-8 is a potent STING agonist with an EC50 of 27 nM in THP1-Dual KI-hSTING-R232 cells (WO2021239068A1, compound 5-AB) .
    STING agonist-8
  • HY-157554
    ZM640

    		NOD-like Receptor (NLR) Inflammation/Immunology
    ZM640 is a NLRP3 inhibitor. ZM640 enhances IL-1β release mediated by NLRP3 inflammasome activation in THP-1 cells. ZM640 shows low cytotoxicity .
    ZM640
  • HY-N7493
    N-acetyldopamine
    1 Publications Verification

    NADA

    		 Endogenous Metabolite TNF Receptor Reactive Oxygen Species (ROS) Others
    N-acetyldopamine is a sepiapterin reductase inhibitor. N-acetyldopamine is a catecholamine that is used by insects as sclerotizing precursors to harden their cuticle. N-acetyldopamine can attenuate LPS-stimulated TNF-α production and superoxide production in THP-1 cells .
    N-acetyldopamine
  • HY-171295
    p38 Kinase inhibitor 7

    		p38 MAPK Inflammation/Immunology
    p38 Kinase inhibitor 7 (Comp:XXXIX) is the inhibitor for p38α with an IC50 of 5.25 nM. p38 Kinase inhibitor 7 inhibits TNFα production in cell THP-1 with an IC50 of 5.88 nM .
    p38 Kinase inhibitor 7
  • HY-173326
    STING-IN-14

    		STING Inflammation/Immunology
    STING-IN-14 is an inhibitor of STING (IC50: 0.6 nM). STING-IN-14 inhibits the activation of the IRF pathway in THP1-Dual TM cells. STING-IN-14 can be used in autoimmune diseases research .
    STING-IN-14
  • HY-131454
    SR-717
    10+ Cited Publications

    		 STING Inflammation/Immunology Cancer
    SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity .
    SR-717
  • HY-145861
    LSD1-IN-14

    		Histone Demethylase Apoptosis Cancer
    LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells .
    LSD1-IN-14
  • HY-170362
    cGAS-IN-4

    		Cyclic GMP-AMP Synthase Inflammation/Immunology
    cGAS-IN-4 (Compound 36) is an orally active inhibitor for cyclic GMP-AMP synthase (cGAS) with IC50 of 32 nM and 5.8 nM for h-cGAS and m-cGAS. cGAS-IN-4 inhibits the cGAMP in THP-1 cell with an IC50 of 60 nM, which improves the cellular potency. cGAS-IN-4 exhibits anti-inflammatory efficacy in Concanavalin A (HY-P2149)-induced acute liver injury in mouse models . orally active, THP-1, C57Bl/6 mouse, orally active
    cGAS-IN-4
  • HY-170529
    NLRP3-IN-61

    		NOD-like Receptor (NLR) Pyroptosis Inflammation/Immunology
    NLRP3-IN-61 (Compound 1) is an inhibitor for NLRP3. NLRP3-IN-61 inhibits pyroptosis in THP-1 cell with an IC50 of 12.6 nM, inhibits IL-β release with an IC50 of 25.3 nM .
    NLRP3-IN-61
  • HY-162588
    MC-ND-18

    		ATTECs NOD-like Receptor (NLR) Inflammation/Immunology
    MC-ND-18 is an ATTEC degrader of NLRP3 through autophagic mechanisms, with the DC50 of 125.5 nM in THP-1 cell. MC-ND-18 is composed of a NLRP3 ligand, linker and LC3 ligand .
    MC-ND-18
  • HY-170530
    NLRP3-IN-62

    		NOD-like Receptor (NLR) Pyroptosis Inflammation/Immunology
    NLRP3-IN-62 (Compound 1) is an inhibitor for NLRP3. NLRP3-IN-62 inhibits pyroptosis in THP-1 cell with an IC50 of 0.7 nM, inhibits IL-β release with an IC50 of 108.5 nM .
    NLRP3-IN-62
  • HY-131454A
    SR-717 free acid
    10+ Cited Publications

    		 STING Inflammation/Immunology Cancer
    SR-717 free acid is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 free acid is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity .
    SR-717 free acid
  • HY-148645
    STING modulator-4

    		STING Inflammation/Immunology
    STING modulator-4 (compound AIH05) is a competitive STING modulator with a Ki of 0.0933 μM for R232H STING. STING modulator-4 has an EC50 of >10 μM for p-IRF3 in THP-1 cell .
    STING modulator-4
  • HY-N8304
    Shegansu B

    (+)-Shegansu B; Parvifolol D

    		 Interleukin Related Inflammation/Immunology
    Shegansu B is an inhibitor of IL-1β. Shegansu B 6 inhibits IL-1β expression on LPS-induced THP-1 cells with 64.74% inhibition. Shegansu B has anti-inflammatory activity .
    Shegansu B
  • HY-15544
    CCR1 antagonist 10

    		CCR Inflammation/Immunology
    CCR1 antagonist 10 (example 1) is a potent and orally active CCR1 antagonist. CCR1 antagonist 10 inhibits 125I-MIP-1α binding to THP-1 cell membranes with an Ki value of 2.3 nM .
    CCR1 antagonist 10
  • HY-14926B
    Levonadifloxacin arginine

    (S)-(-)-Nadifloxacin arginine; WCK 771 arginine

    		 Bacterial Infection
    Levonadifloxacin ((S)-(-)-Nadifloxacin; WCK 771) arginine is a broad-spectrum antistaphylococcal agent. Levonadifloxacin arginine has antimicrobial activity against methicillin-sensitive Staphylococcus aureus (MSSA) and methicillin-resistant Staphylococcus aureus and reduces phagocytosis of MRSA and MSSA strains by monocytic THP-1 cells .
    Levonadifloxacin arginine
  • HY-149816
    Anti-inflammatory agent 41

    		Interleukin Related TNF Receptor NF-κB Inflammation/Immunology
    Anti-inflammatory agent 41 (13a) significantly inhibit lipopolysaccharide (LPS)-induced expression of the proinflammatory cytokines IL-6 and TNF-α on J774A.1, THP-1 and LX-2 cells, and inhibits the activation of the NF-κB pathway .
    Anti-inflammatory agent 41
  • HY-148643
    STING modulator-5

    		STING Inflammation/Immunology
    STING modulator-5 (compound 38) is a STING modulator with a pIC50 value of 9.5. STING modulator-5 antagonizes peripheral blood mononuclear cells (PBMC) with a pIC50 value of 8.1. STING modulator-5 is a antagonist of THP-1 cells, it can be used for immunological disease research .
    STING modulator-5
  • HY-172529
    DPP9-IN-1

    		Dipeptidyl Peptidase Neurological Disease Metabolic Disease
    DPP9-IN-1 (Compound 42) is a dipeptidyl peptidase 9 (DPP9) inhibitor with IC50 of 3 nM for DPP9 and 0.6 μM for DPP8. DPP9-IN-1 induces concentration-dependent LDH release in THP-1 cells .
    DPP9-IN-1
  • HY-156415
    NLRP3 agonist 2

    		NOD-like Receptor (NLR) Inflammation/Immunology
    NLRP3 agonist 2 (compound 22) is a orally active NLRP3 agonist.NLRP3 agonist 2 activates Caspase-1 in THP1 cells .
    NLRP3 agonist 2
  • HY-W014605
    Diphenylcyclopropenone

    Diphencyprone

    		 Interleukin Related Apoptosis p38 MAPK IRE1 Inflammation/Immunology Cancer
    Diphenylcyclopropenone (Diphencyprone) is a potent hapten acting as a topical immunomodulatory agent, which induces an allergic contact dermatitis. Diphenylcyclopropenone induces an increase of cell-surface thiols in cells of a human monocytic cell line, THP-1. Diphenylcyclopropenone acts on the autoreactive T-lymphocytes within the follicular milieu to induce Apoptosis. Diphenylcyclopropenone can be used for alopecia areata research .
    Diphenylcyclopropenone
  • HY-148606
    STING modulator-3

    		STING Cancer
    STING modulator-3 is a STING inhibitor. STING modulator-3 inhibits R232 STING with an Ki value of 43.1 nM in scintillation proximity assay. STING modulator-3 has no effect on IRF-3 activation or TNF-β induction in THP-1 cells .
    STING modulator-3
  • HY-158711
    STING agonist-38

    		STING Cancer
    STING agonist-38 (compound 58) is a potent agonist of STING, with the EC50 of 0.05 μM in THP1 cells. STING agonist-38 has certain oral bioactivity .
    STING agonist-38
  • HY-W080443
    O-allylvanillin

    		Endogenous Metabolite Others Cancer
    O-allylvanillin is O-allylchalcone derivative with anti-cancer effects . O-allylvanillin inhibits THP-1, HL60, Hep-G2, MCF-7 cells growth with IC50 values of 74.76 μM, 63.52 μM, 90.99 μM, and 90.11 μM, respectively .
    O-allylvanillin
  • HY-170364
    NLRP3-IN-60

    		NOD-like Receptor (NLR) Pyroptosis Inflammation/Immunology
    NLRP3-IN-60 (Compound 39) is the orally active inhibitor for NLRP3. NLRP3-IN-60 inhibits pyroptosis with an IC50 of 13 nM in THP-1 cell. NLRP3-IN-60 inhibits IL-1β release with an IC50 of 225 nM in human whole blood .
    NLRP3-IN-60

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