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THP-1cells

" in MedChemExpress (MCE) Product Catalog:

42

Inhibitors & Agonists

1

Peptides

7

Natural
Products

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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 [1].
    CAY10602
  • 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 [1].
    RP23618
  • 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 [1].
    Gypsogenin 3-O-glucuronide
  • 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 [1].
    NLRP3 agonist 2
  • 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 [1].
    STING agonist-38
  • 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 [1].
    CU-32
  • 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 [1].
    Sibiricine
  • HY-168554
    STING-IN-10

    		STING Inflammation/Immunology
    STING-IN-10 (P8) is a dual STING degrader and inhibitor with aDC50 value of 2.58 μM in THP-1 cells. STING-IN-10 has anti-inflammatory activity [1].
    STING-IN-10
  • 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 [1].
    ZM640
  • HY-149781
    STING agonist-34

    		STING Cancer
    STING agonist-34 (Compound 12L) is a potent STING agonist with an IC50 value of 1.15 μM and an EC50 of 0.38 μM in THP1 cells. STING agonist-34 could be used in cancer research [1].
    STING agonist-34
  • HY-120048
    NBC19

    		NOD-like Receptor (NLR) Inflammation/Immunology
    NBC19 is an NLRP3 inflammasome inhibitor with an IC50 of 60 nM in differentiated THP1 cells. NBC19 inhibits nigericin- and ATP-induced IL-1β release with IC50s of 80 nM and 850 nM, respectively [1].
    NBC19
  • HY-162588
    MC-ND-18

    		NOD-like Receptor (NLR) Inflammation/Immunology
    MC-ND-18 is a NLRP3 degrader 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 [1].
    MC-ND-18
  • 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 [1].
    STING modulator-4
  • HY-122941
    Viscidulin II

    		Others 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 [1].
    Viscidulin II
  • 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 [1].
    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 [1].
    CCR1 antagonist 10
  • HY-N7489
    β-Hederin

    		Parasite Infection Inflammation/Immunology
    β-Hederin, a saponin isolated from Hedera helix L.(Araliaceae), possesses antileishmanial activity. β-Hederin exhibits IC50 values of 1.5 μM, 68 nM and 4.57 μM in L. Mexicana promastigotes, L. mexicana amastigotes and THP1 cells, respectively [1] .
    β-Hederin
  • 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 [1].
    LSD1-IN-14
  • 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 [1].
    AZ 11645373
  • 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 [1].
    Levonadifloxacin arginine
  • HY-161671
    GAT2711

    		nAChR Neurological Disease
    GAT2711 (compound 3h) is a full agonist of α9 nAChR with an EC50 of 230 nM. GAT2711 inhibits ATP-induced IL-1β release in THP-1 cells and exhibits analgesic activity in α7 knockout mice [1].
    GAT2711
  • 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 [1].
    STING modulator-3
  • HY-146584
    Cathepsin C-IN-5

    		Cathepsin Inflammation/Immunology
    Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC50s of 59.9 nM, 4.26 µM, >5 µM, >5 µM, >5 µM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serine proteases). Cathepsin C-IN-5 shows anti-inflammatory activity [1].
    Cathepsin C-IN-5
  • HY-18739
    Phorbol 12-myristate 13-acetate
    Maximum Cited Publications
    316 Publications Verification

    PMA; TPA; 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 [1] . Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells .
    Phorbol 12-myristate 13-acetate
  • 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 [1].
    STING modulator-5
  • HY-131945
    CU-115
    2 Publications Verification

    		 Toll-like Receptor (TLR) Inflammation/Immunology
    CU-115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU-115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells [1].
    CU-115
  • 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 [1].
    NOD2 antagonist 1
  • HY-155463
    NLRP3-IN-25

    		NOD-like Receptor (NLR) Interleukin Related Inflammation/Immunology
    NLRP3-IN-25 (compound 32) is an orally available NLRP3 inhibitor with anti-inflammatory activity. NLRP3-IN-25 attenuates renal injury in doxorubicin-induced glomerulonephritis in mice. NLRP3-IN-25 inhibits IL-1β secretion in THP-1 cells with an IC50 of 21 nM [1].
    NLRP3-IN-25
  • HY-P2036A
    FSL-1 TFA
    3 Publications Verification

    		 Toll-like Receptor (TLR) MMP HSV Antibiotic Infection
    FSL-1 TFA, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection [1]. FSL-1 TFA induces MMP-9 production through TLR2 and NF-κB/AP-1 signaling pathways in monocytic THP-1 cells .
    FSL-1 TFA
  • HY-155151
    RIPK2/3-IN-1

    		RIP kinase Inflammation/Immunology
    RIPK2/3-IN-1 is a potent dual RIPK2/3 kinases inhibitor with IC50 values of 3 nM and 117 nM, respectively. RIPK2/3-IN-1 is against RIPK2 with IC50 value 14 nM in 14-TriLAN-Gly/NOD1 THP-1 cell-based NF-κB reporter assay [1].
    RIPK2/3-IN-1
  • 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 [1].
    AS-183
  • HY-164765
    NLRP3-IN-56

    		NOD-like Receptor (NLR) Inflammation/Immunology
    NLRP3-IN-56 (compound 062) is a NLRP3 inhibitor. NLRP3-IN-56 potently inhibits the level of IL-1β secretion by THP-1 cells with an IC50 of 9.7 nM. NLRP3-IN-56 can be used for the study of NLRP3-mediated symptoms and/or diseases [1].
    NLRP3-IN-56
  • HY-159718
    NLRP3-IN-46

    		NOD-like Receptor (NLR) Inflammation/Immunology
    NLRP3-IN-46 (Compound 3k) activates neuro-immunomodulatory cholinergic anti-inflammatory pathway, and thus inhibits NLRP3 inflammasome activation. NLRP3-IN-46 inhibits Uric acid sodium (HY-B2130A)-induced IL-1β production in THP-1 cells, and can be used in gouty arthritis research [1].
    NLRP3-IN-46
  • HY-123942
    Diprovocim
    5 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 [1] .
    Diprovocim
  • HY-162647
    PI3Kδ-IN-22

    		PI3K Inflammation/Immunology
    PI3Kδ-IN-22 (Compound 26) is a selective inhibitor for PI3Kδ with pKi of 9.3. PI3Kδ-IN-22 inhibits PI3Kδ-AKT signaling pathway in THP-1 cells, with pIC50 of 9.4. PI3Kδ-IN-22 exhibits good pharmacokinetic characters in rats [1].
    PI3Kδ-IN-22
  • HY-130481
    Propargyl-PEG4-acid

    		PROTAC Linkers Cancer
    Propargyl-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-IAP PROTACs Ibrutinib (HY-10997)-based PROTAC 2 and an analogue PROTAC 3. PROTAC 3 causes BTK degradation with a DC50 of 200 nM in THP-1 cells [1]. Propargyl-PEG4-acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Propargyl-PEG4-acid
  • HY-131040
    NLRP3-IN-NBC6

    		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) [1].
    NLRP3-IN-NBC6
  • 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 [1].
    PROTAC IRAK4 degrader-8
  • 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 [1].
    NLRP3-IN-49
  • HY-100401A
    Pactimibe sulfate

    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 [1]. 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
    Pactimibe

    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 [1]. 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-159719
    NLRP3-IN-51

    		NF-κB Inflammation/Immunology
    NLRP3-IN-51 (Compound 3q) is a potent cholinergic anti-inflammatory pathway (CAP) activators. ANLRP3-IN-51 inhibits Monosodium urate (MSU) (HY-B2130A)-induced IL-1β production in THP-1 cells, indicating its potential against gout arthritis. NLRP3-IN-51 inhibits MSU induced phosphorylation of NF-κB p65, without any inhibitory effect against NLRP3, pro-caspase 1, or the self-cleavage and activation of caspase-1 of the second signaling. Therefore, NLRP3-IN-51 inhibits the initial phase of NLRP3 through CAP activation [1].
    NLRP3-IN-51

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