Immunology and Inflammation

NLRP3-IN-56 (compound 062) is an inhibitor of NLRP3. It effectively suppresses the secretion of IL-1β in THP-1 cells, demonstrating an IC50 of 9.7 nM. NLRP3-IN-56 is useful for research into NLRP3-mediated symptoms and/or diseases.

mPGES1-IN-9 (compound 1_8) is an mPGES1 inhibitor with an IC50 of 0.5 μM and is utilized in anti-inflammatory research.

NLRP3-IN-58 (Compound DS15) acts as an inhibitor of NLRP3 inflammasome activation, with an IC50 value of 3.85 μM, and is capable of inhibiting 33% of IL-1β release at a concentration of 10 μM.

Glutathione monoethyl ester, a derivative of glutathione, can protect motor neuron cells (NSC-34) from TDP-43 pathology caused by mutations, which includes reducing aggregate formation, nuclear clearance, reactive oxygen species (ROS) production, and cell death.

Ocipumaltib (Example 2) is an inhibitor of mucosa-associated lymphoid tissue protein 1 (MALT1). It functions as an antineoplastic agent and is utilized in the study of cancer, infections, neurological disorders, and hematological diseases.

NP3-146 sodium is an inhibitor of the NLRP3 inflammasome.

Antioxidant agent-3 shows strong DPPH and ABTS+ radical scavenging (IC50: 26.58, 30.31 μM). Boosts ROS, SOD, GSH; lowers LDH in H2O2-exposed HepG2 cells.

Factor B-IN-3 is a potent inhibitor of complement factor B. Factor B-IN-3 can be used to study inflammatory and immune-related diseases.

Heme Oxygenase-1-IN-3 (compound 4) serves as a potent and selective inhibitor of heme oxygenase-1 (HO-1) with a dissociation constant (Kd) of 141 nM, making it suitable for use in cancer and neurodegenerative disease research.

Balsalazide disodium is an aminosalicylate prodrug that releases mesalamine in the colon, providing diverse anti-inflammatory effects in regions affected by colitis. Additionally, it exhibits anticancer properties by modulating the IL-6/STAT3 pathway.

Izicopan (INF056) is an antagonist of the complement factor C5a receptor. It inhibits C5a-induced calcium mobilization with an IC50 ranging from 10 to 100 nM.

TLR7/8 agonist 13 is an orally active dual agonist of TLR7 (with a lowest effective concentration (LEC) [hTLR7] of 1.6 μM) and TLR8 (LEC [hTLR8] of 1.6 μM). It acts on human peripheral blood mononuclear cells (hPBMC) with agonistic activity (LEC [hPBMC] = 0.5 μM). In mice and cynomolgus monkeys, TLR7/8 agonist 13 induces endogenous IFNα, activates myeloid dendritic cells and monocytes, promoting their differentiation towards a TH1 phenotype. In chronic AAV-HBV mouse models, it reduces viral load and HBV surface antigen levels. TLR7/8 agonist 13 has the potential to indirectly induce IFNγ, facilitating the response of HBV antigen-specific CD8 T cells. This compound is useful for hepatitis B virus research.

Pelecopan (BCX9930), an oral complement factor D inhibitor, prevents hemolysis in PNH (IC50=14.3 nM).

Compound WK692 (compund WK692) is a BCL6 inhibitor that effectively suppresses the growth of diffuse large B-cell lymphoma cells without toxic side effects and acts synergistically with inhibitors of EZH2 and PRMT5.

NLRP3-IN-7 (Compound 36) is a selective inhibitor of the NLRP3 inflammasome and is able to assemble the NLRP3 inflammasome.

IKZF2-degrader 1 (Compound 31) is a molecular glue-type degrader of IKZF2 with a DC50 of 0.5 nM. It exhibits relatively low degradation activity against CK1α, with a DC50 of 210 nM. This compound is applicable in research focused on IKZF2-dependent cancers.

G108 is an inhibitor of human cGAS and is used in the study of autoimmune diseases associated with human cGAS.

VISTA-IN-3 (Compound A4), a potent small molecule inhibitor of VISTA, exhibits a dissociation constant (K D) of 0.49 μM. This compound effectively induces the release of IFN-γ cytokines and demonstrates synergistic enhancement of anti-cancer activity when combined with PD-L1 antibody [1].

IRAK4-IN-19, an IRAK4 inhibitor (IC50: 4.3 nM), hampers IL23 synthesis and arthritis progression.