MCC7840, a sulfonylurea, is a potent and selective inhibitor of NLRP3 inflammasome, with an IC50 of <100 nM. MCC7840 can be used for the research of inflammatory diseases.

Z8779877149 (Z7149) is a blood-brain barrier-permeable multi-target ligand that targets SERT (Ki=198 nM), α2A adrenergic receptor (Ki=180 nM; EC50=440 nM) and 5-HT2A receptor (EC50=172 nM, Emax=76%). Z8779877149 inhibits 5-HT reuptake and activates Gi and Gq protein signaling pathways, respectively. Z8779877149 effectively alleviates pain responses as well as depression- and anxiety-like behaviors, while exhibiting favorable safety without inducing sedation or motor impairment. Z8779877149 is available for the research of pain, depression and anxiety disorders.

WMK-1 is a 1,2,4,5-tetraoxane derivative and ferroptosis inducer, with significantly higher cytotoxicity against cancer cells than non-cancerous cells. WMK-1 triggers ferroptosis in cancer cells and cancer stem cells. WMK-1 can be used for the research of cancer.

PROTAC LRRK2 Degrader-2 is a PROTAC-based degrader targeting LRRK2 with a DC50 of 0.14 nM. PROTAC LRRK2 Degrader-2 recruits LRRK2 or its mutants to the cereblon E3 ubiquitin ligase, thereby mediating the targeted ubiquitination and subsequent proteasomal degradation of LRRK2. PROTAC LRRK2 Degrader-2 can be used in research related to Parkinson's disease.

N-Desmethyl xanomeline is a pharmacologically active metabolite of Xanomeline. N-Desmethyl xanomeline binds to muscarinic, serotonergic, histaminergic and dopaminergic receptors. N-Desmethyl xanomeline can be used for the research of schizophrenia.

Brosuximide is a succinimide-type antiepileptic agent.

FK565 is an immunoactive peptide and a nucleotide-binding oligomerization domain (Nod)-1 ligand agonist.

MCC950 (CP-456773) sodium is a potent, selective, small-molecule inhibitor of NLRP3 with IC50 of 7.5 nM in BMDMs.

Sebrinoflast (Compound 5) is a NLRP3 inhibitor with an IC50 ≤1  μM for hNLRP3. Sebrinoflast can be used for inflammatory and cardiovascular diseases including NASH and atherosclerosis and neurological diseases like Alzheimer's disease research.

IIIM-1266 is a NLRP3 inflammasome inhibitor. IIIM-1266 inhibits IL-1β release in mouse macrophages (J774A.1 cells) (IC50 = 2.3 μM) and significantly reduced the protein expression level of mature IL-1β. IIIM-1266 can be used for the study of inflammation.

JNJ-79883960 is a NLRP3 inhibitor. JNJ-79883960 can be used for the study of inflammation.

BAL-1516 is a brain-penetrant and highly selective NLRP3 inhibitor (IC50=14.2 nM). BAL-1516 significantly suppresses IL-1β and IL-18 release in microglial neuroinflammation models (IC50=11-59 nM). BAL-1516 is promising for research of neurodegenerative diseases (e.g., Alzheimer’s, Parkinson’s) and systemic inflammatory disorders.

NP3-742 is an orally active NLRP3 inhibitor that binds to the NLRP3 NACHT domain. NP3-742 inhibits IL-1β release with IC50s of 6 nM and 47 nM in both the cellular and whole blood assays, respectively. NP3-742 is highly selective against a panel of more than 50 enzymes, receptors and sodium and calcium channels. NP3-742 can be used for the study of gout, cardiovascular disease or osteoarthritis.

GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells.

VEN-02XX is an orally active and brain-permeable NLRP3 inhibitor. VEN-02XX inhibits the release of IL-1β and IL-18 (IC50 0.3 and 0.28 μM, respectively). VEN-02XX restores memory and cognition, inhibits microgliosis, and reduces neuroinflammation and tau pathology in the 5XFAD/Rubicon KO mouse model. VEN-02XX may be used in the study of Alzheimer's disease (AD).

NP3-253 is an NLRP3 inhibitor with oral activity and blood-brain barrier permeability, and NP3-253 can serve as a tool to further investigate the biological characteristics of NLRP3 in peripheral and neuroinflammatory model.

HNW005 is a dual inhibitor of NLRP3 inflammasome and urate transporter 1 (URAT1). It has a KD value of 204.6 nM and an IC50 of 1.7 μM for inhibiting NLRP3 inflammasome activation, and an IC50 of 6.4 μM for inhibiting uric acid transmembrane transport. When administered at a dose of 2 mg/kg in vivo, HNW005 can achieve a uric acid reduction rate of 64.8%. It can exert anti - inflammatory, analgesic, and uric acid - lowering activities by inhibiting the activation of NLRP3 inflammasome and uric acid transmembrane transport. HNW005 can be used in the research of gouty arthritis.

JC124 is a specific NLRP3 inflammasome inhibitor. JC124 has anti-inflammatory and neuroprotective effects.

DFV890 (IFM-2427) is apotent, selective and orally active inhibitor of NLRP3 inflammasome, directly binds to NLRP3 and locks the protein in an inactive conformation,prevents NLRP3 inflammasome assembly in response to sterile danger signals.

MCC7840 sodium, a sulfonylurea, is a potent and selective inhibitor of NLRP3 inflammasome, with an IC50 of <100 nM. MCC7840 sodium can be used for the research of inflammatory diseases.

Selnoflast (example 6) is a NLRP3 inhibitor (extracted from patent WO2019008025).

ZYIL1 is an oral small molecule NLRP3 inflammasome inhibitor, exhibits potent (IC50 in nanomolar range) in human whole blood and supresses inflammation caused by the NLRP3 inflammasome.

NP3-146 is a small molecule NLRP3 inflammasome inhibitor and an analog of MCC950.

NLRP3-inhibitory compound 7 (NIC7) is a small-molecule inhibitor of Nod-like receptor family pyrin domain-containing 3 (NLRP3), inhibits NLRP3-mediated activation of caspase 1 along with the secretion of IL-1β, IL-18, and lactate dehydrogenase.

NDT-19795 is the carboxylic acid metabolite of selective NLRP3 inhibitor NT-0796, suppresses release of IL-1β in LPS-activated human PBMCs with IC50 of 47 nM.

ML146 (ML-146, Pubmed CID-1088438) is a selective small molecule NOD1 inhibitor with IC50 of 1.5 uM in NOD1 agonist-stimulated NF-κB reporter assay in HEK293T cells.

JT002 is a potent and selective inhibitor of NLRP3 inflammasome with IC50 of 6 nM (IL-1β production from hPBMCs), inhibits NLRP3 mediated cytokine production and pyroptosis.

JT001 (JT-001) is a potent, highly specific NLRP3 inhibitor, inhibits NLRP3 inflammasome assembly.

JC2-11 is an anti-inflammasome compound and a pan-inhibitor of the NLRP3, NLRC4, and AIM2 inflammasomes.

FK156 is an immunoactive peptide and a nucleotide-binding oligomerization domain (Nod)-1 ligand agonist.