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THP-1

" in MedChemExpress (MCE) Product Catalog:

192

Inhibitors & Agonists

3

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17

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2

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1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-132221

    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-18739
    Phorbol 12-myristate 13-acetate
    Maximum Cited Publications
    389 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-169917

    Drug Derivative Cancer
    THP-1/MV-4-11 against-1 (compound 12k) is an anticancer agent with potency inhibitory against THP-1/MV/4 cells (IC50=29 nM and 98 nM, respectively). THP-1/MV-4-11 against-1 is one of 5-substituted thiazolyl urea derivatives, can be used in leukemic diseases research [1].
    THP-1/MV-4-11 against-1
  • HY-123270

    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-171295

    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 [1].
    p38 Kinase inhibitor 7
  • HY-170529

    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 [1].
    NLRP3-IN-61
  • HY-N12469

    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-170530

    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 [1].
    NLRP3-IN-62
  • HY-167877

    p38 MAPK Inflammation/Immunology
    PS-166276 is a highly potent and less cytotoxic inhibitor of p38. PS166276 has an IC50 of 28 nM at p38 kinase and 170 nM in the THP-1 TNFα assay [1].
    PS-166276
  • HY-170362

    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 [1]. orally active, THP-1, C57Bl/6 mouse, orally active
    cGAS-IN-4
  • HY-157554

    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-N8304

    (+)-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-145861

    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-159718

    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-14926A

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

    Antibiotic Bacterial Infection
    Levonadifloxacin (arginine) hydrate is a broad-spectrum anti-staphylococcal agent. Levonadifloxacin (arginine) hydrate shows antibacterial activity against Methicillin (HY-121544)-susceptible Staphylococcus aureus (MSSA) and Methicillin-resistant S. aureus (MRSA) strains, with a reduction of which phagocytized in THP-1 monocytes [1].
    Levonadifloxacin (arginine) hydrate
  • HY-108670

    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-161325

    Parasite Infection
    Antileishmanial agent-26 (Compound 69) is a guanidine-containing compound with anti-Leishmania donovani activity. Its IC50 value against Leishmania donovani is 5.67 μM, and its CC50 value against THP-1 is 3.79 μM. Antileishmanial agent-26 can be used in the research of tropical diseases [1].
    Antileishmanial agent-26
  • 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-14926

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

    Antibiotic Bacterial Infection
    Levonadifloxacin ((S)-(-)-Nadifloxacin; WCK 771) is a broad-spectrum anti-staphylococcal agent. Levonadifloxacin shows antibacterial activity against Methicillin (HY-121544)-susceptible Staphylococcus aureus (MSSA) and Methicillin-resistant S. aureus (MRSA) strains, with a reduction of which phagocytized in THP-1 monocytes [1].
    Levonadifloxacin
  • HY-116926

    Antibiotic Bacterial DNA/RNA Synthesis Topoisomerase Apoptosis Infection Cancer
    Deoxynybomycin is an antibiotic, that can be isolated from Streptomyces, and antibacterial activity against Staphylococcus aureus. Deoxynybomycin is the inhibitor for DNA gyrase and Topoisomerase I. Deoxynybomycin induces expression of p21/WAF1, exhibits cytotoxicity and induces apoptosis in cancer cells Saos-2, TMK-1, and THP-1 [1] .
    Deoxynybomycin
  • HY-W080443

    Endogenous Metabolite Others Cancer
    O-allylvanillin is O-allylchalcone derivative with anti-cancer effects [1]. 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 [1].
    O-allylvanillin
  • HY-122941

    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 [1].
    Viscidulin II
  • HY-162647

    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-163280

    NAMPT Neurological Disease
    JGB-1-155 is a positive allosteric modulators (N-PAMs), which enhances the activity of nicotinamide phosphoribosyltransferase NAMPT with EC50 of 3.29 μM. JGB-1-155 counteracts the oxidative stress, through upregulating the NAD + in THP-1 human monocytes. JGB-1-155 attenuates TNFα-induced ROS in HT-22 cells [1].
    JGB-1-155
  • HY-168554

    PROTACs STING Inflammation/Immunology
    STING-IN-10 (P8) is a dual STING PROTAC degrader and inhibitor with a DC50 value of 2.58 μM in THP-1 cells. STING-IN-10 has anti-inflammatory activity [1].(Pink: Target protein ligand (HY-168676); Black: linker (HY-W123015); Blue: E3 ligase ligand (HY-126457))
    STING-IN-10
  • HY-147506

    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-146581

    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 [1].
    Cathepsin C-IN-4
  • HY-146580

    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 [1].
    Cathepsin C-IN-3
  • 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 [1].
    Glutaminyl cyclases-IN-1
  • HY-134375

    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 [1].
    cAIMP
  • HY-129340

    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-135453

    Bacterial Infection
    (-)-Pinocembrin exhibits anti-mycobacterium activity against mycobacteriuum tuberculosis H37Ra with an IC50 value of 1.11 mg/mL in dormant phase and 1.21 mg/mL in active phase, respectively. (-)-Pinocembrin has potent antiproliferative activity with IC50 values of 1.88-11.00 mg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines [1].
    (-)-Pinocembrin
  • 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-155245

    CDK Bcl-2 Family Cancer
    A09-003 is a CDK-9 inhibitor (IC50: 16 nM). A09-003 inhibits leukemia cell proliferation (IC50: 1.90, 0.86, 2.49, 1.84, 0.48 μM for BDCM, Molm-14, THP-1, U937, MV4-11 cells). A09-003 induces apoptosis and decreases Mcl-1 expression through Thr163 dephosphorylation [1].
    A09-003
  • HY-P10694

    Bacterial Infection Inflammation/Immunology
    IDR-HH2 is an immunomodulatory peptide with the ability to modulate the host cytokine/chemokine environment. IDR-HH2 can promote the adhesion of monocytes and THP-1 cells to fibronectin. Additionally, IDR-HH2 possesses antibacterial activity, inhibiting the activity of both P. aeruginosa and S. aureus with MIC values of 75 µg/mL and 38 µg/mL, respectively [1] .
    IDR-HH2
  • HY-144168A

    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 [1].
    STING agonist-8 dihydrochloride
  • HY-N8390

    Others Cancer
    3-Epidehydropachymic acid, a lanostane triterpenoid, shows totoxicity effect against human acute monocytic leukemia cell line THP-1 (IC50=52.51 μM) [1].
    3-Epidehydropachymic acid
  • HY-153673

    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-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-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) [1].
    PPARα/γ agonist 3
  • HY-158434

    IRAK Inflammation/Immunology
    IRAK1-IN-1 (compound B8) is an orally active IRAK1 inhibitor. IRAK1-IN-1 inhibits the release of IL-6 with the IC50 values of 4.57 μM and 6.51 μM on mouse cells J774A. 1 and human cells THP-1, respectively. IRAK1-IN-1 alleviats LPS (HY-D1056)-induced acute lung injury (ALI) and DSS(HY-116282C)-induced colitis in mice [1].
    IRAK1-IN-1
  • HY-172208

    PROTACs Cyclic GMP-AMP Synthase Inflammation/Immunology
    PROTAC cGAS degrader-1 (Compound TH35) is an effective and selective cGAS PROTAC degrader, with DC50 values of 0.9 μM and 4.6 μM in THP-1 and RAW 264.7 cells, respectively. PROTAC cGAS degrader-1 can inhibit the activation of cGAS signaling induced by dsDNA. PROTAC cGAS degrader-1 has anti-inflammatory activity and can be used in the research of cGAS-related inflammatory diseases. (Pink: cGAS inhibitor (HY-133916); Black: Linker (HY-W411604); Blue: E3 ligase ligand (HY-43722)) [1]
    PROTAC cGAS degrader-1
  • HY-N12186

    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-144168

    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) [1].
    STING agonist-8
  • 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. [1].
    NLRP3-IN-57
  • 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 [1].
    SR-717
  • HY-146283

    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 [1].
    LSD1-IN-18
  • HY-146284

    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 [1].
    LSD1-IN-19
  • 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 [1].
    SR-717 free acid
  • HY-162588

    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 [1].
    MC-ND-18

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