nigericin

Nigericin is a polyether antibiotic with potent antimicrobial, antimalarial, anticoronaviral and anticancer activities. It is capable of promoting cellular potassium efflux, inducing Caspase-1/GSDMD and Caspase-3-mediated cellular pyroptosis and apoptosis in triple-negative breast cancer, and inducing apoptosis in PEL (primary exudative lymphoma) cells through mitochondrial dysfunction and Wnt/β-catenin signaling downregulation.

Nigericin sodium salt is an antibiotic, an NLRP3 activator, and a cationic ion carrier. Nigericin sodium triggers the activation of the NALP3 inflammasome, which inhibits Golgi function and suppresses the growth of Gram-positive bacteria.

NLRP3/AIM2-IN-3 is a unique molecule that inhibits NLRP3 and AIM2 inflammasome activation in a species-specific manner. It has an IC50 value for cell lysis of 0.077 ± 0.008 μ M. NLRP3/AIM2-IN-3 is a potent inhibitor of NLRP3 and AIM2 inflammasome-dependent cell lysis with an IC50 value for cell lysis of 0.077 ± 0.008 μ M. NLRP3/AIM2-IN-3 inhibits LPS/nigericin NLRP3/AIM2-IN-3 inhibits LPS/nigericin-stimulated cell lysis in THP-1 macrophages with an IC50 value of 0.077 ± 0.008 μM. NLRP3/AIM2-IN-3 interferes with the interaction of NLRP3 or AIM2 with the bridging protein ASC, inhibiting oligomerization of ASC.

ADS032 (BT-032) is an NLRP1 and NLRP3 inhibitor with anti-inflammatory activity,, inhibits the activation of NLRP1 and NLRP3, inhibits Nigericin-induced IL-1β production, and can be used to study respiratory inflammation or infection.

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].

NLRP3-IN-57 (compound 5) inhibits the NLRP3 inflammasome, consequently downregulating IL-1β levels in THP-1 macrophages induced by LPS+Nigericin.

NLRP3-IN-81 (N102) is an inhibitor capable of crossing the blood-brain barrier, effectively countering NLRP3 inflammasome-dependent pyroptosis with an EC50 of 0.029 μM for Nigericin-induced pyroptosis. It significantly suppresses caspase-1 activation and IL-1β release that depend on NLRP3. Additionally, NLRP3-IN-81 disrupts the interaction between NLRP3 and the adaptor protein ASC, while inhibiting ASC oligomerization. This compound is applicable in research on pyroptosis-related diseases, such as inflammatory bowel disease and type 2 diabetes.

NLRP3-IN-86 (Compound 8a), a derivative of Songorine, is a potent and selective inhibitor of the NLRP3 inflammasome. It effectively reduces lactate dehydrogenase (LDH) release induced by LPS and Nigericin, with an IC50 of 2.69 μM in THP-1 cells and 1.75 μM in J774A.1 cells. Additionally, NLRP3-IN-86 inhibits the cleavage of gasdermin D (GSDMD) and the secretion of IL-1β, effectively suppressing pyroptosis. This compound is applicable for inflammation-related research.

A-130A is a polycyclic polyether compound belonging to the nigericin group of antibiotics generated by Streptomyces hygroscopicus strain.

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.

Potent NLRP3 inflammasome inhibitor (IC50 = 60-80 nM). Inhibits nigericin- and ATP-induced IL-1β release. Baldwin et al (2017) Boron-Based Inhibitors of the NLRP3 Inflammasome. Cell Chem.Biol. 24 1321 PMID:28943355 |Redondo-Castro et al (2018) Development of a characterised tool kit for the interrogation of NLRP3 inflammasome-dependent responses. Sci.Rep. 8 5667 PMID:29618797

Azalamellarin N is a pyroptosis inhibitor that exhibits varying inhibitory effects on different pyroptosis inducers. It functions by targeting molecules upstream of NLRP3 inflammasome activation, instead of directly affecting the components of the NLRP3 inflammasome. Its inhibitory potency against various inducers is ranked as follows: Nigericin > R837 [1].

NLRP3-IN-28 (compound N77) serves as a potent inhibitor of NLRP3, effectively blocking Nigericin-induced pyroptosis with an EC50 of 0.07μM. Additionally, it mitigates inflammatory reactions in vivo [1].