Pyroptosis

Disulfiram (TETD) is an inhibitor of the acetaldehyde dehydrogenase ALDH, inhibiting hALDH1 and hALDH2 (IC50=0.15 1.45 μM) with specificity. Disulfiram is acutely sensitized to alcohol and also inhibits GSDMD pore formation.

LDC7559 inhibits gasdermin D (GSDMD) by blocking neutrophil extracellular trap (NET) at late stage.

Ac-YVAD-CMK (Ac-Tyr-Val-Ala-Asp-CMK) is a selective and irreversible inhibitor of Caspase-1 and inhibits pyroptosis, IL-1β and IL-18. Ac-YVAD-CMK shows neuroprotective and anti-inflammatory capacity.

1. Polyphyllin VI has hemostasis , expectorant , bacteriostasis, anticytotoxic, anti pregnancy kill sperm effects.

Apilimod 2HCl (STA 5326 2HCl) is a PIKFYVE kinase inhibitor that promotes NLRP3 inflammatory vesicle activation, IL-1β secretion, and cellular pyroptosis, and is used in the study of amyotrophic lateral sclerosis.

1,7-Diphenyl-4-hepten-3-one is a compound isolated from Alpinia officinarum, which activates the Nrf2 pathway to suppress pyroptosis. It alleviates cognitive impairment and pathological damage in APP PS1 mice and prevents oxidative stress damage while reducing levels of pyroptosis-related proteins. 1,7-Diphenyl-4-hepten-3-one enhances Aβ-induced proliferation in HT22 cells and can be used in Alzheimer’s disease research.

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.

Morroniside would act as a regulator of hepatic inflammatory reactions and lipid metabolism in db db mice. It exhibits protective effects against diabetic renal damage and human umbilical vein endothelial cells, by inhibiting hyperglycemia and oxidative s

Ac-FEID-CMK TFA is a selective zebrafish GSDMEb-derived peptide inhibitor that reduces mortality and renal injury in infectious shock. It inhibits pyroptosis in vivo, attenuates septic AKI (acute kidney injury), and inhibits the caspy2-mediated atypical inflammatory vesicle pathway.

Caspase-3 activator 1 (compound 4b), a Ru(III) metal complex, effectively inhibits gastric tumor growth and metastasis by mediating caspase-3 cleavage, enabling Caspase-3 to process gasdermin E (GSDME), resulting in GSDME-N terminus production and perforation of the gastric tumor cell membrane. Furthermore, compound 4b induces pyroptosis and subsequent immune responses and can be incorporated with decitabine (DCT) into the 4b-DCT-Lip lipid delivery system [1].

NLRP3-IN-55 (Compound 19) is an effective inhibitor of NLRP3, exhibiting an inhibitory concentration (IC50) of 0.34 μM. It targets the NLRP3 protein directly with a dissociation constant (KD) of 0.45 μM, effectively blocking the assembly and activation of the NLRP3 inflammasome. This action results in anti-inflammatory effects and inhibits cell pyroptosis.

CIB-1476, a caspase-1 inhibitor, effectively reduces joint swelling in mouse models of arthritis and demonstrates lasting anti-inflammatory effects. This compound achieves its benefits by blocking IL-1β production, NF-κB activation, and GSDMD-mediated pyroptosis, all of which are triggered by the NLRP3 inflammasome.

ICy-Q, a near-infrared (NIR) reagent activated by quinone oxidoreductase 1 (NQO-1), interacts with NQO-1 to yield the reduced product ICy-OH. This derivative selectively triggers pyroptosis and resultant death in pancreatic cancer cells. Moreover, ICy-Q serves as a valuable instrument for the expedited and precise diagnosis of intraoperative pathological sections [1].