thp-1 cells

NLRP3-IN-9 (INF-4E) is an inhibitor of NLRP3 ATPase and caspase-1. NLRP3-IN-9 acts by irreversibly trapping thiol nucleophiles, which prevents both ATP- and nigericin-triggered pyroptosis of human THP-1 cells in a time- and concentration-dependent manner.

2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) is a second messenger in cellular innate immunity, catalyzed by cGAMP synthase (cGAS) under DNA binding conditions. It binds to STING to form a dimer, inducing the production and expression of interferon-β and other cytokines.

Adezmapimod (SB 203580) is a selective, ATP-competitive p38 MAPK inhibitor (IC50=0.3-0.5 μM) that activates autophagy and mitochondrial autophagy, with more than 100-fold higher selectivity over PKB, LCK, and GSK-3β.

Romidepsin (FR 901228) is an HDAC inhibitor that inhibits HDAC1 2 4 6 (IC50=36 47 510 1400 nM). Romidepsin has antitumor activity and can be used for the treatment of peripheral T-cell lymphoma and cutaneous T-cell lymphoma.

2-Deoxy-D-glucose (2-DG) is an analog of glucose, an inhibitor of glycolysis. 2-Deoxy-D-glucose has antiviral activity, as well as inhibitory cell proliferation and apoptosis-inducing activity.

Emricasan (IDN-6556) is a pan-caspase inhibitor with irreversible properties. Emricasan has anti-inflammatory and anti-apoptotic activity and can be used in the treatment of infections and liver failure, etc. Emricasan also inhibits Zika virus infections.

Lsd1-in-20 is a potent dual inhibitor of LSD1 G9a with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 showed antiproliferative activity against THP-1 leukemia cells and MDA-MB-231 breast cancer cells in vitro, with IC50 of 0.51 and 1.60 μM, respectively, at 72 h.

CU-115 is a selective and potent TLR8 antagonist with IC50 of 1.04 µM and =>50 µM for TLR8 and TLR7, respectively. CU-115 decreases production of TNF-α and IL-1β activated by R-848 in THP-1 cells.

NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor with an IC50 of 574 nM. It acts independently of Ca 2+ and inhibits Nigericin-induced inflammasome activation in THP-1 cells, as well as Imiquimod-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs) [1].

Rifampicin (Rifamycin AMP) is a broad-spectrum antibiotic. Rifampicin has a strong antibacterial effect against Mycobacterium tuberculosis and is also effective against gram-positive and gram-negative bacteria and viruses.

Ursolic acid (Prunol) is a natural product, a pentacyclic triterpene carboxylic acid extracted from Rhododendron caprifolium. Ursolic acid has anti-tumor, anti-inflammatory, anti-bacterial and hypoglycemic activities.

Lovastatin (MK-803) is an HMG-CoA reductase inhibitor (IC50=3.4 nM). Lovastatin lowers cholesterol and is commonly used as a lipid-lowering agent in the treatment of hypercholesterolemia.

α-Vitamin E (Dexrabeprazole Sodium) is a naturally-occurring form of vitamin E, a fat-soluble vitamin with potent antioxidant properties.

C29 is a novel inhibitor of TLR2 1 and TLR2 6 signaling induced by synthetic and bacterial TLR2 agonists in human HEK-TLR2 and THP-1 cells, but only TLR2 1 signaling in murine macrophages.

CAY10602 is a SIRT1 activator derived from high throughput screening for compounds that enhance SIRT1-mediated deacetylation of a SIRT1-specific substrate. Functional assays indicate that CAY10602 dose-dependently suppresses NF-κB-dependent induction of TNF-α by lipopolysaccharide in THP-1 cells, achieving approximately 75% inhibition at 60 μM without cytotoxicity.

Neriifolin (17β-Neriifolin), a cardiac glycoside extracted from the unripe fruit of Cerbera manghas, is a Na+K+-ATPase inhibitor with anticancer activity that inhibits cell proliferation by suppressing HOXA9-dependent gene expression and inducing apoptosis in the human acute myeloid cell line, THP-1. Neriifolin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells and can be used in prostate cancer research.

CCX140 (CCX140-B) (CCX140-B) is an antagonist of CCR2.

Manumycin A is an antibiotic with anticancer activity and is a mammalian thioredoxin reductase-1 (TrxR-1) inhibitor.Manumycin A inhibits the production of IL-1β, IL-6, and IL-8 in TNF alpha-stimulated THP-1 cells and peripheral blood mononuclear cells in a dose-dependent manner, inducing apoptosis.

Propargyl-PEG4-acid is a PEG-based PROTAC linker used in the synthesis of BTK-IAP PROTACs, including Ibrutinib-based PROTAC 2 and its analogue PROTAC 3. PROTAC 3 induces BTK degradation with a DC50 of 200 nM in THP-1 cells[1].

NLRP3-IN-49 (compound Z48) is a potent and specific inhibitor of NLRP3, displaying IC50 values of 0.26 μM in THP-1 cells and 0.21 μM in mouse bone marrow-derived macrophages. It directly binds to the NLRP3 protein with a dissociation constant (Kd) of 1.05 μM, effectively preventing the assembly and activation of the NLRP3 inflammasome, thereby exhibiting anti-inflammatory properties. NLRP3-IN-49 is utilized in the research of inflammatory bowel disease.

NLRP3-IN-46 (Compound 3k) activates the cholinergic anti-inflammatory pathway involved in neuro-immune modulation, thereby inhibiting the activation of the NLRP3 inflammasome. Furthermore, NLRP3-IN-46 suppresses the production of IL-1β in THP-1 cells induced by Uric acid sodium, making it relevant for research in gouty arthritis.

NLRP3-IN-51 (Compound 3q) is an effective activator of the cholinergic anti-inflammatory pathway (CAP). This compound demonstrates potential for treating gouty arthritis as it inhibits the production of IL-1β in THP-1 cells induced by monosodium urate (MSU). Furthermore, NLRP3-IN-51 suppresses the phosphorylation of NF-κBp65 triggered by MSU without impacting the self-cleavage and activation of NLRP3, pro-caspase 1, or the second messenger caspase-1. Therefore, the initial stage of NLRP3 inhibition by NLRP3-IN-51 occurs through the activation of CAP.

STING-IN-10 (P8) serves as both a dual degrader and inhibitor of STING, exhibiting an impressive DC50 value of 2.58 μM in THP-1 cells. This compound also demonstrates anti-inflammatory activity.

NLRP3-IN-56 (compound 062) is an inhibitor of NLRP3. It effectively suppresses the secretion of IL-1β in THP-1 cells, demonstrating an IC50 of 9.7 nM. NLRP3-IN-56 is useful for research into NLRP3-mediated symptoms and or diseases.