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

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THP-1 cells

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Acyltransferase (3) Antibiotic (2) Apoptosis (6) Aryl Hydrocarbon Receptor (1) Bacterial (3) Bcl-2 Family (2) c-Fms (3) Cathepsin (2) CCR (2) CDK (1) Cyclic GMP-AMP Synthase (1) Dihydroorotate Dehydrogenase (1) Dipeptidyl Peptidase (1) DNA/RNA Synthesis (2) Epigenetic Reader Domain (3) Glucocorticoid Receptor (2) HDAC (1) Histone Demethylase (4) Histone Methyltransferase (1) HIV (1) HSV (1) Interleukin Related (4) IRAK (3) Keap1-Nrf2 (1) Mitochondrial Metabolism (1) MMP (1) nAChR (1) NAMPT (1) NF-κB (4) NOD-like Receptor (NLR) (13) P2X Receptor (1) p38 MAPK (1) Parasite (1) Phospholipase (1) PI3K (1) PKC (1) PROTAC Linkers (1) PROTACs (3) RIP kinase (3) Sirtuin (1) SphK (1) Src (1) STING (12) TNF Receptor (4) Toll-like Receptor (TLR) (4) Topoisomerase (1) Wnt (2)
By Research Areas:	Cancer (32) Cardiovascular Disease (3) Endocrinology (2) Infection (8) Inflammation/Immunology (51) Metabolic Disease (1) Neurological Disease (4)
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-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 . Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells .

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-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-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 .

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-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-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 .

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-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 .

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-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 .

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 (K_d=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 .

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-168554

STING-IN-10	STING	Inflammation/Immunology
STING-IN-10 (P8) is a dual STING degrader and inhibitor with a DC₅₀ value of 2.58 μM in THP-1 cells. STING-IN-10 has anti-inflammatory activity .

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) .

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-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 .

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 .

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-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 .

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-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 .

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 .

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-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 .

HY-W080443

O-allylvanillin	Others	Others Cancer
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-116926

Deoxynybomycin	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 .

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 .

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-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 .

HY-162658

Leuxinostat	HDAC Apoptosis	Cancer
Leuxinostat is an inhibitor for HDAC with IC₅₀ of 30 nM for hHDAC6. Leuxinostat inhibits the proliferation of cells THP1, K562, U937 and MEK1, induces apoptosis in leukemia cells NB4 and MOLT-4. Leuxinostat inhibits the expansion of hematopoietic stem cells and exhibits antileukemic activity in zebrafish models .

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-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 .

Cat. No.	Product Name	Target	Research Area

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 .

Cat. No.	Product Name		Classification

HY-130481

Propargyl-PEG4-acid		PROTAC Synthesis Alkynes
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.

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THP-1 cells

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