Pyroptosis Inhibitor

Garlic oil (synthetic) is an orally effective anti-inflammatory, antioxidant, and anticancer agent. Garlic oil (synthetic) inhibits the activation of NF-κB, NFκB2 and NLRP3 inflammasome, and induces the expression of GSTA1, HO-1 and NQO-1. Garlic oil (synthetic) reduces the Bcl-2/Bax protein ratio and activates NNK-induced apoptosis (apoptosis) in lung tissues. Garlic oil (synthetic) attenuates NNK-induced apoptosis in MRC-5 cells and reduces excessive ROS production. Garlic oil (synthetic) alleviates pyroptosis (pyroptosis) and exerts a protective effect against acute lung injury in mice. Garlic oil (synthetic) inhibits lung tumorigenesis in mice and improves small intestinal motility in rats with type 2 diabetes. Garlic oil (synthetic) can be used in research related to acute lung injury, lung cancer, peptic ulcer, type 2 diabetes and hypertension.

NLRP3-IN-26 (compound 15Z) is a NLRP3 inhibitor with the IC₅₀ of 0.13 μM. NLRP3-IN-26 can be used for DSS-induced colitis model study.

Ciliatoside A is a naturally bioactive compound that exhibits significant anti-inflammatory, antiviral, and neuroprotective activities. Ciliatoside A serves as a mitophagy inducer and NLRP3 inflammasome inhibitor, activating AMPK, SIRT1, and the PINK1/Parkin axis, and inhibiting pyroptosis and apoptosis. Ciliatoside A promotes autophagic flux, autophagosome-lysosome fusion, mTOR inhibition, and p62-dependent HBc degradation; reduces Aβ aggregation, plaque deposition, microglial/astrocyte activation, and bacterial load; and maintains neuronal integrity, mitochondrial membrane potential, and ATP production. Ciliatoside A is used in research on Alzheimer's disease, Klebsiella pneumoniae-induced pneumonia, hepatitis B virus infection, and inflammation.

NLRP3-IN-60 (Compound 39) is the orally active inhibitor for NLRP3. NLRP3-IN-60 inhibits pyroptosis with an IC₅₀ of 13 nM in THP-1 cell. NLRP3-IN-60 inhibits IL-1β release with an IC₅₀ of 225 nM in human whole blood.

Relaxin H3 (human) is a relaxin peptide with anti-inflammatory, anti-apoptotic, anti-pyroptotic, anti-migratory, protective and anti-fibrotic activities. Relaxin H3 (human) acts on RXFP1 to generate cAMP and reduce the levels of ATP and ROS. Relaxin H3 (human) inhibits renal inflammatory pyroptosis (pyroptosis), NLRP3 inflammasome activation, caspase-1 activation, IL-1β/IL-18 secretion, collagen synthesis, TGF-β1 signaling pathway, Smad2 phosphorylation, myofibroblast differentiation, TIMP expression, and HRMEC migration. Relaxin H3 (human) activates AMPK, upregulates MFN2 expression, improves mitochondrial quality control and membrane potential, inhibits apoptosis (apoptosis) and pyroptosis, restores retinal ultrastructure, and reverses excessive left ventricular collagen expression. Relaxin H3 (human) can be used in studies related to kidney stones, nephrocalcinosis, diabetic cardiomyopathy, fibrotic cardiomyopathy, and diabetic retinopathy.

Chiisanogenin is an orally active triterpenoid. Chiisanogenin reduces postprandial blood glucose by promoting GLUT4 translocation and glucose uptake via activation of the IRS-1/PI3K/Akt signaling pathway. Chiisanogenin binds to MLKL and inhibits its phosphorylation and oligomerization, maintains lysosomal integrity, restores autophagic flux, and suppresses NLRP3 inflammasome activation and pyroptosis. Chiisanogenin inhibits xanthine oxidase activity and regulates oxidative stress and ion pump activity. Chiisanogenin binds to or inhibits PKA, H⁺/K⁺-ATPase and β-glucuronidase. Chiisanogenin possesses multiple pharmacological activities, including broad-spectrum antibacterial activity, anticancer, anti-inflammatory, antirheumatic, renoprotective, cardioprotective and antiarrhythmic effects. Chiisanogenin can be used in research related to type 2 diabetes, rheumatoid arthritis, myocardial injury, hepatocellular carcinoma and ventricular arrhythmia^.

Thromycin (Standard) is the analytical standard of thromycin (Acetopyrrothin) (HY-N6712). Thiolutin is a sulfur-containing antibiotic, which is a potent inhibitor of bacterial and yeast RNA polymerases. Thiolutin can be produced by Streptomyces. Thiolutin inhibits AMSH (IC₅₀ = 4 μM) and Rpn11 (IC₅₀ = 0.53 μM). Thiolutin is a dual inhibitor of BRCC36 and the NLRP3 inflammasome, exhibiting anti-inflammatory effects. Thiolutin effectively suppresses the interaction between BRCC36 and HMGCR, leading to the inhibition of HCC growth. Thiolutin attenuates pyroptosis and NLRP3 inflammasome activation. Thiolutin markedly alleviates renal injury and inflammatory process in IgAN. Thiolutin is an anti-angiogenic compound which can ease Doxorubicin (HY-15142A)-induced cardiotoxicity (DOXIC)^{[1][2][3][4][5]}.

ECDD-S16 is a potent inhibitor of pyroptosis. ECDD-S16 inhibits surface and endosomal TLR ligands activated pyroptosis in Raw264.7 cells.

Necrosulfonamide (Standard) is the analytical standard of Necrosulfonamide (HY-100573). This product is intended for research and analytical applications. Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.

LDC7559 (Standard) is the analytical standard of LDC7559 (HY-111674). This product is intended for research and analytical applications. LDC7559 is a gasdermin D (GSDMD) inhibitor via blocK_ing neutrophil extracellular trap (NET) in the late stages .

Triptophenolide (Standard) (Hypolide) is the analytical standard of Triptophenolide (HY-N0475). This product is intended for research and analytical applications. Triptophenolide is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC₅₀ of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer.

Lenalidomide-d₄ (CC-5013-d₄) is the d₄-labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013) is an orally active immunomodulatory agent that binds CRBN as a molecular glue to alter substrate specificity, inducing ubiquitination and proteasome-dependent degradation of IKZF1, IKZF3 and CK1α. Lenalidomide induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide promotes IL-2 release and effector functions of CD8⁺ T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide can be used in research related to hematological malignancies, acute liver failure and acute kidney injury.

Periplogenin (Standard) is the analytical standard of Periplogenin (HY-N2414). Periplogenin is an orally active cardiac glycoside found in Cortex periplocae. Periplogenin can induce ROS production and necroptosis and cause G0/G1 phase arrest. Periplogenin can inhibit pyroptosis by regulating the NLRP3/Caspase-1/GSDMD signaling. Periplogenin suppresses growth of prostate carcinoma cells by docking to an ATP1A1 protein pocket and forming a hydrogen bond with T804. Periplogenin can be used for the researches of cancer, inflammation and immunology, such as prostate carcinoma, rheumatoid arthritis and psoriasis.

2-Bromohexadecanoic acid (Standard) is the analytical standard of 2-Bromohexadecanoic acid (HY-111770). This product is intended for research and analytical applications. 2-Bromohexadecanoic acid (2-Bromopalmitate; 2-BP) is a palmitoylation inhibitor targeting DHHC (Asp-His-His-Cys) protein palmitoyltransferase. 2-Bromohexadecanoic acid inhibits palmitoylation of GSDME-C during pyroptosis and inhibits BAK/BAX-Caspase 3-GSDME pathway-mediated pyroptosis.

Sipeimine (Standard) is the analytical standard of Sipeimine (HY-N0696R). Sipeimine (Imperialine) is an inhibitor targeting the PI3K/AKT/NF-κB pathway and NLRP3 inflammasome, which can competitively bind to PI3K and p65. Sipeimine inhibits PI3K/AKT phosphorylation, blocks NF-κB nuclear translocation and NLRP3 inflammasome activation. Sipeimine exerts anti-inflammatory activities, inhibits pyroptosis and ferroptosis, and protects the extracellular matrix. Sipeimine can reduce cartilage degradation and synovial inflammation in osteoarthritis and improve PM2.5-induced lung injury. Sipeimine is mainly used in the study of anti-inflammatory and degenerative diseases.

Sweroside (Standard) is the analytical standard of Sweroside (HY-N0806). This product is intended for research and analytical applications. Sweroside is an iridoid glycoside that targets multiple targets, including the Keap1/Nrf2 axis, NLRP3 inflammasome, SIRT1, NF-κB, AMPK/mTOR pathway, and caspase family. Sweroside promotes Nrf2 nuclear translocation by competitively binding to Keap1. Sweroside also inhibits oxidative stress and NLRP3-mediated pyroptosis by activating Nrf2, inhibits NF-κB inflammatory pathway by activating SIRT1, and promotes autophagy and induces caspase-dependent apoptosis via the AMPK/mTOR pathway. Sweroside has antioxidant, anti-inflammatory, anti-apoptotic, and lipid metabolism regulating activities, and can be used in the research of myocardial ischemia-reperfusion injury, leukemia, acute lung injury, non-alcoholic fatty liver disease, and other fields.

INF200 (compound 5) is a sulfonylurea-based inhibitor of NLRP3 and NLRP3-mediated pyroptosis. INF200 has beneficial cardiometabolic effects in rat model of high-fat diet (HFD)-induced metaflammation，and shows anti-inflammatory activity to (10 μM) decreases IL-1β release in human macrophages. INF200 improves glucose and lipid profiles，and attenuates systemic inflammation and biomarkers of cardiac dysfunction (particularly BNP). INF200 also improves myocardial damage-dependent ischemia/reperfusion injury (IRI) in hemodynamic evaluation.

NLRP3-IN-28 (compound N77) is a potent inhibitor of NLRP3. NLRP3-IN-28 inhibits Nigericin (HY-127019)-induced pyroptosis with an EC₅₀ of 0.07μM. NLRP3-IN-28 alleviates the inflammatory reaction in vivo.

Garlic oil is an orally effective anti-inflammatory, antioxidant, and anticancer agent. Garlic oil inhibits the activation of NF-κB, NFκB2 and NLRP3 inflammasome, and induces the expression of GSTA1, HO-1 and NQO-1. Garlic oil reduces the Bcl-2/Bax protein ratio and activates NNK-induced apoptosis (apoptosis) in lung tissues. Garlic oil attenuates NNK-induced apoptosis in MRC-5 cells and reduces excessive ROS production. Garlic oil alleviates pyroptosis (pyroptosis) and exerts a protective effect against acute lung injury in mice. Garlic oil inhibits lung tumorigenesis in mice and improves small intestinal motility in rats with type 2 diabetes. Garlic oil can be used in research related to acute lung injury, lung cancer, peptic ulcer, type 2 diabetes and hypertension.