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THP-1 NLuc

" in MedChemExpress (MCE) Product Catalog:

366

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9

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

    PMA; TPA; Phorbol myristate acetate

    		 PKC SphK NF-κB Neurological Disease Inflammation/Immunology Cancer
    Phorbol 12-myristate 13-acetate (PMA; TPA; Phorbol myristate acetate), 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 (Validated by MedChemExpress (MCE)) .
    Phorbol 12-myristate 13-acetate
  • HY-N7038
    Phytohemagglutinin
    5+ Cited Publications

    PHA-M

    		 NF-κB COX Interleukin Related Reactive Oxygen Species (ROS) Neurological Disease Inflammation/Immunology Cancer
    Phytohemagglutinin (PHA-M), the major seed lectin of the common bean, Phaseolus vulgaris, is a T-cell activator. Phytohemagglutinin stimulates human mononuclear leukocytes, inducing the expression of ChAT mRNA and potentiating ACh synthesis. Phytohemagglutinin induces dose- and time-dependent toxicity in THP-1 monocytes/macrophages, alters cellular morphology, causes organelle dysfunction, and increases the expression of NF-κB, COX2, IL-1β [1] .
    Phytohemagglutinin
  • HY-131454
    SR-717
    25+ 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-123942
    Diprovocim
    10+ Cited Publications

    		 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-P2036A
    FSL-1 TFA
    4 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-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-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 [1] .
    N-acetyldopamine
  • HY-131454A
    SR-717 free acid
    25+ 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-172208
    PROTAC cGAS degrader-1

    		PROTACs Cyclic GMP-AMP Synthase Inflammation/Immunology
    PROTAC cGAS degrader-1 is a potent 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 induces proteasome-mediated degradation of cGAS, inhibits the cGAS signaling pathway, and attenuates double-stranded DNA-induced activation of cGAS in human and mouse cells. PROTAC cGAS degrader-1 is applicable to research related to ulcerative colitis [1].
    PROTAC cGAS degrader-1
  • 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 [1] .
    Diphenylcyclopropenone
  • HY-163159
    NP3-562

    		NOD-like Receptor (NLR) Interleukin Related Inflammation/Immunology
    NP3-562 is an orally active NLRP3 Inhibitor. NP3-562 inhibits IL-1β release in the supernatant of Nigericin (HY-127019)-stimulated THP-1 cells (IC50 = 66 nM), human whole blood (IC50 = 214 nM) and a mouse acute peritonitis model. NP3-562 can be used for the study of acute peritonitis [1].
    NP3-562
  • HY-100688
    ML390
    1 Publications Verification

    		 Dihydroorotate Dehydrogenase Cancer
    ML390 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor. ML390 is an inducer of myeloid differentiation and causes myeloid differentiation in murine (ER-HoxA9) and human (U937 and THP1) acute myeloid leukemia (AML) models [1] .
    ML390
  • 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
    Levonadifloxacin

    (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-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-175764
    FIP22

    		PROTACs IRAK NF-κB p38 MAPK TNF Receptor Interleukin Related Inflammation/Immunology
    FIP22 is a potent and selective IRAK4 PROTAC degrader (HEK293T cells: DC50 = 3.2 nM; THP-1 cells: DC50 = 10.6 nM). FIP22 induces the ubiquitin-proteasome system by forming an IRAK4-FIP22-CRBN ternary complex (EC50 = 12.63 nM), thereby potently blocking IRAK4-mediated NF-κB and MAPK signaling pathways. FIP22 can be used for the study of atopic dermatitis (Pink: IRAK4 ligand (HY-175765); Blue: CRBN ligand (HY-W087383); Black: Linker (HY-46871)) [1].
    FIP22
  • HY-174455
    APH02174

    		PROTACs IRAK Interleukin Related Inflammation/Immunology
    APH02174 is a highly selective and orally active IRAK4 PROTAC degrader with the DC50 of 4.01 nM in THP-1 cells. APH02174 blocks inflammatory signals by inhibiting IL-6 release. APH02174 can be used for research on inflammatory conditions such as psoriasis vulgaris and rheumatoid arthritis [1].
    APH02174
  • 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 [1]. orally active, THP-1, C57Bl/6 mouse, orally active
    cGAS-IN-4
  • HY-175167
    diABZI-i

    		STING IFNAR Inflammation/Immunology
    diABZI-i is an orthogonal STING inhibitor. diABZI-i significantly inhibits cGAMP-induced IFNβ in PBMCs. diABZI-i also activates constitutive signaling of V155M SAVI and exerts potent agonistic effects in the STING V155M THP-1 cell model. diABZI-i can be used for research on monogenic autoinflammatory diseases such as SAVI [1].
    diABZI-i
  • HY-162588
    MC-ND-18

    		NOD-like Receptor (NLR) ATTECs Autophagy Inflammation/Immunology
    MC-ND-18 is an ATTEC degrader that degrades NLRP3 via the Autophagy pathway, with a DC50 of 125.5 nM in THP-1 cells. MC-ND-18 exhibits anti-inflammatory activity in a DSS-induced mouse model of colitis. MC-ND-18 can be used for research on inflammatory bowel disease. MC-ND-18 consists of an NLRP3 inhibitor (HY-156121), a linker (HY-W018745), and an LC3 ligand [1].
    MC-ND-18
  • HY-122623A
    DB818 dihydrochloride

    		Apoptosis Cancer
    DB818 dihydrochloride is the dihydrochloride salt form of DB818 (HY-122623). DB818 dihydrochloride is an inhibitor for Homeobox A9 (HOXA9). DB818 dihydrochloride reduces the formation of HOXA9-DNA complexes, inhibits the growth and induces apoptosis in AML cell lines OCI/AML3, MV4-11, and THP-1 [1].
    DB818 dihydrochloride
  • HY-161671
    GAT2711

    		nAChR Neurological Disease Inflammation/Immunology
    GAT2711 is a full agonist of α9 nAChR with an EC50 of 230 nM. GAT2711 shows 340-fold selective for α9 over α7 nAChRs. GAT2711 inhibits ATP-induced IL-1β release in THP-1 cells. GAT2711 retains full analgesic activity in α7 nAChR knockout mice [1].
    GAT2711
  • HY-163280
    JGB-1-155

    		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-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-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-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-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-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-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-151132
    Glutaminyl cyclases-IN-1

    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
    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 [1].
    cAIMP
  • 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)) [1].
    MS2133
  • 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) [1].
    3-Epidehydropachymic acid
  • 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) [1].
    STING agonist-8
  • HY-W750678
    9-cis-Canthaxanthin

    		Apoptosis Caspase Inflammation/Immunology
    9-cis-Canthaxanthin is a carotenoid with pro-apoptotic activity in THP-1 macrophage cells. 9-cis-Canthaxanthin induces cell apoptosis by increasing caspase-3 and caspase-8 activity [1].
    9-cis-Canthaxanthin
  • 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 [1].
    DPP9-IN-1
  • 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-171953
    THP1 Lipid

    		Liposome Others
    THP1 Lipid is an ionizable lipidoid. THP1 Lipid can be used to synthesize lipid nanoparticles (LNPs) for delivering mRNA to muscles with minimal toxicity and editing genes in specific liver tissues in tdTomato transgenic mice model. THP1 Lipid can be used for vaccine delivery and CRISPR/Cas9-mediated gene editing research [1].
    THP1 Lipid
  • HY-168554
    STING-IN-10

    		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-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 [1].
    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 [1].
    Cathepsin C-IN-3
  • 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 [1].
    STING agonist-8 dihydrochloride
  • HY-175003
    HV1-IN-2

    		Proton Pump 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 [1].
    HV1-IN-2
  • 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-172217
    DNMT1-IN-5

    		DNA Methyltransferase Apoptosis Cancer
    DNMT1-IN-5 (Compound 55) is the inhibitor for DNMT that inhibits DNMT1 and DNMT3A with IC50 of 2.42 μM and 14.4 μM. DNMT1-IN-5 exhibits antiproliferative activity in a variety of cancer cell lines (IC50s for TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226 and HCT116 are 0.19-2.37 μM), arrests the cell cycle at G2/M phase, and induces apoptosis in TMD-8 and DOHH2 cells. DNMT1-IN-5 exhibits antitumor efficacy in TMD-8 xenograft mouse models [1].
    DNMT1-IN-5
  • 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-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-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 [1].
    p38 Kinase inhibitor 7
  • 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 [1].
    NLRP3-IN-61
  • 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

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