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THP-1cells

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By Targets:	Acyltransferase (1) Antibiotic (1) Apoptosis (1) Cathepsin (1) CCR (1) Histone Demethylase (1) HSV (1) Interleukin Related (2) MMP (1) NF-κB (2) NOD-like Receptor (NLR) (6) P2X Receptor (1) p38 MAPK (1) Parasite (1) PKC (1) PROTAC Linkers (1) RIP kinase (1) Sirtuin (1) SphK (1) STING (4) TNF Receptor (1) Toll-like Receptor (TLR) (3)
By Research Areas:	Cancer (5) Cardiovascular Disease (1) Infection (2) Inflammation/Immunology (20) Metabolic Disease (1)
Click Chemistry:	PROTAC Synthesis (1) Alkynes (1)

Inhibitors & Agonists

Peptides

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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].

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].

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	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].

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].

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].

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].

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].

HY-148645

STING modulator-4	STING	Inflammation/Immunology
STING modulator-4 (compound AIH05) is a competitive STING modulator with a K_i of 0.0933 μM for R232H STING. STING modulator-4 has an EC₅₀ of >10 μM for p-IRF3 in THP-1 cell ^[1].

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].

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].

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 K_i value of 2.3 nM ^[1].

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] .

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].

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].

HY-148606

STING modulator-3	STING	Cancer
STING modulator-3 is a STING inhibitor. STING modulator-3 inhibits R232 STING with an K_i 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].

HY-18739

Phorbol 12-myristate 13-acetate Maximum Cited Publications 243 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 .

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].

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].

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].

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].

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].

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 .

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].

HY-123942

Diprovocim 2 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] .

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.

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].

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 K_i 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 .

HY-100401

Pactimibe CS-505 free base
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 K_i 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 .

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 .

Gypsogenin 3-O-glucuronide	Structural Classification Ketones, Aldehydes, Acids Source classification Gypsophila paniculata Linn . Plants Caryophyllaceae	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].

Sibiricine	Structural Classification Alkaloids Source classification Corydalis crispa Prain Plants Isoquinoline Alkaloids Papaveraceae	Others
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].

Viscidulin II	Structural Classification Flavonoids Scutellaria baicalensis Georgi Flavones Labiatae Source classification Plants	Others
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].

Shegansu B (+)-Shegansu B; Parvifolol D	Structural Classification Source classification Gnetum parvifolium (Warb.) C. Y. Cheng ex Chun Phenols Polyphenols Gnetaceae Plants	Interleukin Related
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].

β-Hederin	Triterpenes Hedera nepalensis K. Koch var. sinensis (Tobl.) Rehd. Classification of Application Fields Terpenoids Source classification Plants Disease Research Fields Inflammation/Immunology Araliaceae	Parasite
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] .

Phorbol 12-myristate 13-acetate 240+ Cited Publications PMA; TPA; Phorbol myristate acetate	Ketones, Aldehydes, Acids Croton tiglium Linn. Source classification Euphorbiaceae Plants Inflammation/Immunology Disease Research Fields	PKC SphK NF-κB
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 .

Propargyl-PEG4-acid		Alkynes PROTAC Synthesis
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.

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THP-1cells

Inhibitors & Agonists

Peptides

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Click Chemistry

Natural
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