inflammasome

BAY 11-7082 (BAY 11-7821) is an NF-κB inhibitor that suppresses TNFα-induced IκBα phosphorylation (IC50=10 μM) and also inhibits the ubiquitin-specific proteases USP7 and USP21 (IC50=0.19/0.96 μM).

Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and no intrinsic sympathomimetic activity.

Carvedilol (SKF 105517) Phosphate is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and devoid of intrinsic sympathomimetic activity. The S enantiomer of carvedilol nonselectively binds to and blocks beta-adrenergic receptors, thereby exerting negative inotropic and chronotropic effects, and leading to a reduction in cardiac output. In addition, both enantiomers of carvedilol bind to and block alpha 1-adrenergic receptors, thereby causing vasodilation and reducing peripheral vascular resistance.

Adrenalone hydrochloride (Adrenalone HCl) is a dopamine β-oxidase inhibitor with a similar structure to the norepinephrine transporter (NET) ligand, with an IC50 of 36.9 μM. It is an adrenergic agonist that acts as a local vasoconstrictor and hemostatic agent.

ATP disodium salt (Adenosine-Triphosphate) is a P2 purinoceptor agonist.

Stavudine (BMY-27857), a nucleoside reverse transcriptase inhibitor analog of thymidine, has activity against HIV.

Muscone (3-Methylcyclopentadecanone) is an organic compound that is the primary contributor to the odor of musk.

NLRP3-IN-2 (5-Chloro-N-(p-sulfamoylphenethyl)-o-anisamide), an intermediate capable of synthesizing glibenclamide, exerts an inhibitory effect on the formation of NLRP3 inflammatory vesicles in cardiomyocytes, limiting infarct size after myocardial ischemia/reperfusion in mice and has no effect on metabolism.

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.

OXSI-2 (Syk Inhibitor) is an inhibitor of Syk with an EC50 of 313 nM and an IC50 of 14 nM. OXSI-2 completely inhibits Adaptor protein LAT Y191 phosphorylation and Syk mediated events in platelets.

CP 424174 is an inhibitor of IL-1β post-translational processing with IC50 of 210 nM. Inhibits the formation of mature IL-1β. Indirectly inhibits NLRP3. Active in vivo and orally bioavailable.

Emlenoflast (MCC7840) is a selective inhibitor of NLRP3 inflammasome.

Arglabin ((+)-Arglabin) is a natural product isolated from Artemisia glabella, is a NLRP3 inflammasome inhibitor, has anti-atherogenic and anticancer effects.

BAA473, a bile acid analog, is a potent activator of the pyrin inflammasome, inducing secretion of interleukin-18 (IL-18) through inflammasome activation in both myeloid and intestinal epithelial cells [1].

Dapansutrile is a potent, selective and orally active NLRP3 inflammasome inhibitor, with Anti-inflammatory and analgesic activity.

hydrocotarnine is an inhibitor of Cbl.

NLRP3-IN-79 (Compound B6) is a selective inhibitor of the NLRP3 inflammasome with an IC50 value of 10.69 nM. It blocks the assembly of the NLRP3 inflammasome by disrupting the interaction between NEK7 and NLRP3. NLRP3-IN-79 shows potential for research in NLRP3-driven inflammatory diseases such as systemic inflammation, peritonitis, and colitis.

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-14 is a potent, selective inhibitor of the NLRP3 inflammasome, displaying a dissociation constant (K D) of 5.87 μM and an IC50 of 0.131 μM for inhibiting IL-1β release. It is applicable for inflammation research.

NLRP3-IN-17 is a potent, selective, and orally active inhibitor of the NLRP3 inflammasome with an IC50 of 7 nM, effectively inhibiting NLRP3-dependent IL-1β secretion in mice, making it valuable for chronic inflammatory disease research [1].

NLRP3-IN-38 (Compound 18) serves as an inhibitor of the NOD-like receptor protein 3 (NLRP3), effectively blocking the activation of the NLRP3 inflammasome with an EC50 value of 23 nM [1].

SBN-284 (compound 3x) acts as a dual inhibitor of cholinesterases (Cholinesterases) and NLRP3 inflammasomes, demonstrating blood-brain barrier permeability. It exhibits IC50 values of 0.37, 0.31, and 0.29 μM against EeAChE, hAChE, and eqBChE respectively, and an EC50 value of 1 μM against NLRP3. SBN-284 is utilized in Alzheimers disease research.

Emlenoflast sodium (MCC7840 sodium), a sulfonylurea, is a selective NLRP3 inflammasome inhibitor with an IC50 value of less than 100 nM for NLRP3 inflammasome, and can be used in the study of inflammatory diseases.

INT-777 (S-EMCA) is a potent, selective TGR5 agonist with an EC₅₀ of 0.82 μM. Following subarachnoid hemorrhage in rats, INT-777 inhibits NLRP5-ASC inflammasome-mediated neuroinflammation via the TGR3/cAMP/PKA signaling pathway. INT-777 exhibits multiple effects, including metabolic regulation, anti-inflammatory activity, cholagogue effects, and vascular protection. INT-777 can be used in research on diseases such as metabolic syndrome, non-alcoholic fatty liver disease, inflammatory bowel disease, and pulmonary arterial hypertension.