NOD-like Receptor (NLR)

Emlenoflast (MCC7840) sodium, a sulfonylurea, is a potent and selective inhibitor of NLRP3 inflammasome, with an IC50 of <100 nM.

BMS-986299 (compound 112) is a first-in-class NLRP3 inflammasome agonist with an EC50 of 1.28 μM.

QS-21 is an immune-stimulatory saponin that can be used as an effective vaccine adjuvant.

Nangibotide TFA is a synthetic peptide and TREM-1 receptor inhibitor.

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

NOD2 antagonist 1 (compound 32) is a potent and selective NOD2 antagonist with an IC50 of 5.23 μM. NOD2 antagonist 1 inhibits Muramyl dipeptide (MDP)-induced IL-8 secretion in THP-1 cells and inhibits MDP-induced IL-6, IL-10, TNF-α release in PBMCs.

GDC-2394 is an orally effective and selective NLRP3 inhibitor that also inhibits IL-1β, with IC50 values of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). GDC-2394 inhibits caspase-1 activity induced by NLRP3, but does not inhibit inflammasome activation dependent on NLRC4.

JC2-11 is an inhibitor of inflammasomes. It inhibits the NLRP3, AIM2, and non-canonical (NC) inflammasomes that contain a recruitment domain protein. JC2-11 reduces the secretion of caspase-1 (p20), cleavage of gasdermin D (GSDMD), and release of IL-1β and lactate dehydrogenase (LDH) in inflammasomes. JC2-11 inhibits the activation of inflammasomes by disrupting the production of reactive oxygen species and the activity of caspase-1.

NLRP3/AIM2-IN-2 is a novel potent inhibitor with species-specific effects on NLRP3 and AIM2 inflammasome-dependent cell pyroptosis, with an IC50 value of 0.2392 ±0.0233μM.

NLRP3-IN-10 is a potent inhibitor of NLRP3 that inhibits IL-1β with an IC50 of 251.1 nM. NLRP3-IN-10 can reduce ASC speck formation and inhibit NLRP3 inflammasome activation.

NLRP3-IN-11 is an inhibitor of the NLRP3 protein. It has biological activity with an IC50 value of

NLRP3-IN-13 (compound C77 in reference patent) is an effective selective NLRP3 inhibitor (IC50: 2.1 μM). It inhibits NLRP3 and NLRC4 inflammasomes, and suppresses IL-1β production mediated by NLRP3. NLRP3-IN-13 also inhibits NLRP3 ATPase activity. It can be used for research on neuroinflammatory diseases.

NLRP3-IN-18 (compound 13) is an effective NLRP3 inhibitor with an IC50 value of ≤ 1.0 µM[1].

β-Aminoarteether (SM934 free base) is an Artemisinin derivative with orally active.

NIC-0102 is an orally active proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation.

NLRP3-IN-17 is a potent, selective and orally active NLRP3 inflammasome inhibitor with an IC50 value of 7 nM.

HMGB1-IN-1 (compound 6) displays strong NO inhibitory effect in RAW264.7 cells with IC50 value of 15.9 ± 0.6 μM.

Usnoflast is a NLRP3 modulator, as well as a non-steroidal anti-inflammatory agent (NSAD).

ADS032 is a dual inhibitor of NLRP1 and NLRP3 that can rapidly, reversibly and stably inhibit inflammasome formation.

NP3-562 is a potent, orally active, tricyclic NLRP3 Inhibitor, with an IC50 of 214 nM.

Antcin A is a potent NLRP3 inhibitor that inhibits the assembly and activation of the NLRP3 inflammasome.

Peptide5 TFA, a connexin 43 mimetic peptide, reduces animals swelling, astrogliosis, and neuronal cell death after spinal cord injury.

M-TriDAP (N-Acetylmuramyl-L-Ala-γ-D-Glu-meso-diaminopimelic acid) is a NOD1/2 agoist and biological active peptide.

NT-0796 is an orally active, selective and CNS-penetrant NLRP3 inflammasome inhibitor.