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Pathways Recommended:	Stem Cell/Wnt Cell Cycle/DNA Damage

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THP-1 cells

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By Targets:	Acyltransferase (1) Antibiotic (1) Apoptosis (2) Aryl Hydrocarbon Receptor (1) Bacterial (1) Bcl-2 Family (2) c-Fms (3) Cathepsin (2) CCR (1) CDK (1) Dihydroorotate Dehydrogenase (1) Dipeptidyl Peptidase (1) DNA/RNA Synthesis (1) Epigenetic Reader Domain (3) Glucocorticoid Receptor (1) Histone Demethylase (4) Histone Methyltransferase (1) HIV (1) HSV (1) Interleukin Related (4) IRAK (1) Keap1-Nrf2 (1) Mitochondrial Metabolism (1) MMP (1) NAMPT (1) NF-κB (3) NOD-like Receptor (NLR) (8) P2X Receptor (1) p38 MAPK (1) Parasite (1) PKC (1) PROTAC Linkers (1) PROTACs (2) RIP kinase (3) Sirtuin (1) SphK (1) STING (9) TNF Receptor (4) Toll-like Receptor (TLR) (4) Wnt (1)
By Research Areas:	Cancer (23) Cardiovascular Disease (1) Endocrinology (1) Infection (5) Inflammation/Immunology (37) Metabolic Disease (1) Neurological Disease (3)
Click Chemistry:	PROTAC Synthesis (1) Alkynes (1)

Inhibitors & Agonists

Peptides

Natural
Products

Click Chemistry

Targets Recommended: Nuclear Factor of activated T Cells (NFAT)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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 .

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 .

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 .

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 .

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 .

HY-146283

LSD1-IN-18	Histone Demethylase	Cancer
LSD1-IN-18 (compound 7) is a potent, non-covalent and selective LSD1 inhibitor, with K_i of 0.156 μM and K_D 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 .

HY-146284

LSD1-IN-19	Histone Demethylase	Cancer
LSD1-IN-19 (compound 29) is a potent, non-covalent and selective LSD1 inhibitor, with K_i of 0.108 μM and K_D 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 .

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 K_i 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 .

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 .

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 .

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) .

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 .

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 .

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	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) .

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 .

HY-131454

SR-717 5+ 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 .

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 .

HY-131454A

SR-717 free acid	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 .

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 .

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 .

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 .

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 .

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 .

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	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 .

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 .

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 . Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells .

HY-W080443

O-allylvanillin	Others	Others
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 .

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 .

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 .

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 .

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 .

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 . 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 .

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 .

HY-135453

(-)-Pinocembrin	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 .

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 .

HY-155245

A09-003	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 .

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 .

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 . 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) .

HY-156622

Leramistat HMC-C-01-A; MBS2320	Mitochondrial Metabolism	Cancer
Leramistat (HMC-C-01-A; MBS2320) is a mitochondrial complex 1 inhibitor, involving in cell metabolism immune metabolism regulation. Leramistat also inhibits ATP production in Thp1 human monocytes (IC₅₀: 0.63 μM). Leramistat inhibits atopic dermatitis and other skin diseases autoimmune diseases, inflammatory diseases, cancer; and also inhibits osteoclast mediated disease .

HY-149522

WK499	Bcl-2 Family Apoptosis	Cancer
BCL6-IN-10 (Compound WK499) is a BCL6 inhibitor. BCL6-IN-10 interrupts the binding of BCL6 to SMRT protein. BCL6-IN-10 induces cell apoptosis, cell cycle arrest and DNA damage. BCL6-IN-10 inhibits AML cell proliferation (IC₅₀s: 0.91, 1.63, 1.026, 7.42, 0.87, 0.85μM for OCl-AML3, THP1, MOLM13, HL60, KG1, NB4 cell respectively) .

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 . 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 . 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 .

HY-112038

GSK2983559 free acid	RIP kinase	Inflammation/Immunology
GSK2983559 free acid (compound 3) is an orally active and potent receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 free acid can block many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples .

HY-112038A

GSK2983559	RIP kinase	Inflammation/Immunology
GSK2983559 is an orally active and potent receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 blocks many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples .

HY-B0415

Fluocinolone (Acetonide)	Glucocorticoid Receptor Wnt	Inflammation/Immunology Endocrinology
Fluocinolone is a glucocorticoid glucocorticoid receptor agonist. Fluocinolone is effective in preventing both lipid accumulation and inflammation. Fluocinolone can promote the proliferation of DPCs and has the potential role in repairing injured pulp tissues. Fluocinolone can be used to study the prevention of chemotherapy-induced peripheral neuropathy caused by Paclitaxel (HY-B0015) .

HY-133131

PROTAC BRD4 Degrader-1	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC₅₀ of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression .

HY-150501

Diprovocim-X	Toll-like Receptor (TLR)	Inflammation/Immunology
Diprovocim-X (compound 35) is a potent TLR1/TLR2 (toll-like receptor 1/2) agonist, with EC₅₀ values of 0.14 and 0.75 nM for hTLR1/TLR2 and mTLR1/TLR2, respectively. Diprovocim-X is a potent adjuvant in vivo in mice, and serves to stimulate the adaptive immune response .

HY-146034

NOD1/2 antagonist-1	NOD-like Receptor (NLR)	Inflammation/Immunology Cancer
NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-binding oligomerization domain-like receptor 1/2) dual antagonist, with IC₅₀ values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T_1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX) .

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THP-1 cells

Inhibitors & Agonists

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