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.

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.

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

NLRP3-IN-77 is a small-molecule NLRP3 inflammasome inhibitor that reduces caspase-1 activation and the release of pro-inflammatory cytokines such as IL-1β by inhibiting the assembly and activation of the NLRP3 inflammasome.

Pactimibe is a ACAT inhibitor. It has anti-atherosclerotic activity.

TMI-1 (WAY-171318), a novel orally active inhibitor of ADAM17 (TACE) and MMP, induces tumor apoptosis in a breast cancer.

VAS 3947 is a specific inhibitor of NADPH oxidase (NOX).VAS 3947 has a potent anti-platelet effect, inducing apoptosis through UPR activation, mainly due to protein aggregation and misfolding, independent of anti-NOX activity.

DY-46-2 is a selective non-nucleoside DNA methyltransferase 3A (DNMT3A) inhibitor (IC50: 0.39 ± 0.23 μM) with anticancer activity for the study of cancer and tumors.

Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor, acting on ACAT1 (IC50: 4.9 μM) and ACAT2 (IC50: 3.0 μM). It inhibits oleoyl-CoA non-competitively (Ki: 5.6 μM) and significantly inhibits cholesterol ester formation (IC50: 6.7 μM). Pactimibe sulfate reduces plasma cholesterol activity and has anti-atherogenic potential.

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.

Alpinone 3-acetate showed anti-inflammatory effects and inhibited the inflammatory response in mouse ear edema models induced by 12-O-tetradecanophenol 13-acetate. Alpinone 3-acetate is a derivative of Alpinone. Alpinone is an active natural compound derived from sunflower with immunomodulatory and antiviral activities.

Phorbol 12-myristate 13-acetate (PMA) is a natural phorbol ester that acts as an activator of PKC, SphK, and NF-κB, and is commonly used to induce differentiation of THP-1 cells and establish dermatitis models.

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].

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].