HS-243 (HS243) is a highly potent, super-selective IRAK-1/4 inhibitor with IC50 of 24/20 nM, respectively.HS-243 shows exquisite potency toward IRAK-1/4 over all other human kinases with only minimal TAK1-inhibiting activity (IC50=0.5 uM).HS-243 binds in the ATP-binding pocket of IRAK-4.HS-243 potently reduces the proinflammatory response of RA cells and macrophages, has distinct cytokine profile from TAK1.HS-243 reduces percentage of survival in pancreatic and breast cancer cell lines.

GSK669 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor, inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling (IC50=0.5 uM), has an IC50 of 3.2 uM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells.GSK669 specifically inhibits MDP-induced NOD2 activation, has no effect on IL-8 secretion induced by over-expression of NOD1.GSK669 significantly inhibits platelet proinflammatory cytokine release induced by muramyl dipeptide, platelet aggregation, ATP release, and ROS generation induced by collagen and collagen related peptide (CRP). GSK669 inhibits thrombosis and oxidative stress via targeting platelet glycoprotein VI (GPVI), decreases malonaldehyde (MDA) and increases superoxide dismutase (SOD) levels in mouse plasma

GNE-2256 (GNE2256) is a potent, selective inhibitor of IRAK4 with biochemical Ki of 1.4 nM.GNE-2256 displays high selectivity in the CEREP panel with off-targets with >50% inhibition are TACR1, HTR2B and ACHE.GNE-2256 is potent in the NanoBRET assay (IC50 = 3.3 nM), the IL-6 human whole blood assay (IC50=190 nM) and the IFNα human whole blood assay (IC50=290 nM).

Evixapodlin is a highly potent, small molecule human PD-1/PD-L1 protein-protein interaction inhibitor with IC50 of 0.213 nM, exhibits potential anticancer and antiviral activities.

DF2593A (DF 2593A) is a potent, selective, noncompetitive allosteric inhibitor of C5aR with IC50 of 5 nM (C5a-induced human PMN migration inhibition), and rat and mouse orthologs (IC50=6.0 nM and IC50=1.0 nM, respectively); dispalys >1,000-fold selective versus other chemoattractants, including CXCL8 and CXCL1 (CI50>10 uM), as well as on a panel of different GPCRs and ion channels; DF2593A demonstrated antinociceptive effects in several models of inflammatory pain and effectively inhibited articular hyperalgesia in CFA-induced mechanical and thermal hyperalgesia and arthritic nociception.

CU-72 is a potent, selective TLR7/8 dual inhibitor with IC50 of 5.10 and 2.87 uM, respectively.

C5 complement inhibitor 7 (C5-IN-7) is a potent, small-molecule inhibitor of C5 complement protein with serum assay IC50 of <5 nM (2% human serum complement inhibition).C5-IN-7 demonstrated excellent potency and good aqueous solubility, inhibited MAC deposition with IC50 of 1 uM in a complement inhibition assay using 50% human whole blood.The C5 triple mutants (C704R, V705I and N707H) were not inhibited by C5 complement protein inhibitor 7 up to 100 uM.C5 complement protein inhibitor 7 binds within the predicted pocket between the C5a and MG8 domains in close proximity to the C5 convertase cleavage site (R751-L752).

BMS-905 is a potent dual inhibitor of TLR7 and TLR8 with IC50 of 0.3 nM (TLR7, IL-6 inhibition in mouse blood), shows good selectivity against TLR9 and other TLR family members.

AMY-101 (Cp40) is a peptidic inhibitor of the central complement component C3 for the management of patients with ARDS caused by SARS-CoV-2 infection.AMY-101 is a novel complement C3-targeted therapeutic based on the 3 rd-generation compstatin analog Cp40.

A-552 (A552) is a potent, small molecule antagonist of human IL-36γ, exhibits Ki of 31/54 nM in the human IL-36γ evoked CXCL1 release in human/mouse cellular assays.A-552 directly binds to human IL-36γ with IC50 of 67.6 nM measured by ITC, does not show affinity for either mouse IL-36γ, human IL-36α or IL-36β.A-552 attenuates human IL-36γ induced chemokine release in mouse plasma, and hIL-36γ induced inflammation in human 3D skin equivalents.A-552 is a novel first in class small molecule antagonist of the IL-36 signaling pathway that binds selective human IL-36γ and can dose-dependently inhibit IL-36γ induced production of proinflammatory cytokines from human and mouse cells.

A potent, selective FLAP inhibitor with binding IC50 of 2.6 nM; inhibits LTB4 synthesis following ionophore challenge in human whole blood with IC50 of 76 nM (5 h incubation); shows good selectivity over CYP3A4, 2C9, and 2D6; exhibits excellent preclinical toxicology, pharmacokinetics and oral bioactivity.

ABC 294640 (ABC294640, Opaganib) is a is a selective, competitive and orally bioavailable sphingosine kinase-2 (SphK-2) inhibitor with IC50 of 60 uM, Ki of 9.8 uM.

iNOs-IN-1 (YPW) is a potent inducible nitric oxide synthase (iNOS) inhibitor. iNOs-IN-1 can significantly inhibit the expression of IL-6 and iNOS, as well as reduce LPS-induced NO generation with dose-dependent manner in mouse macrophages. Anti-inflammatory effects.

8A8 is a potent proinflammatory factor NO inhibitor with an IC50 of 4.7 μM. 8A8 also significantly inhibits LPS-induced HaCat cell proliferation.

IL-17 modulator 6 (compound 61) is a potent Interleukin 17 (IL-17) modulator (pIC50=9.1). IL-17 modulator 6 has the ability to inhibit IL-17 and can be used for the treatment of inflammatory and autoimmune diseases.

Anti-inflammatory agent 10 (compound 30) is a tilomisole-based benzimidazothiazole derivative. Anti-inflammatory agent 10 expresses activity on COX-2 enzyme more than COX-1. Anti-inflammatory agent 10 is orally active.

Anti-inflammatory agent 9 (compound 28) is a tilomisole-based benzimidazothiazole derivative. Anti-inflammatory agent 9 expresses activity on COX-2 enzyme more than COX-1. Anti-inflammatory agent 9 is orally active.

Anti-inflammatory agent 8 (compound 13) is a tilomisole-based benzimidazothiazole derivative. Anti-inflammatory agent 8 expresses activity on COX-2 enzyme more than COX-1 with an IC50 of 0.09 nM. Anti-inflammatory agent 8 is orally active.

Tepoxalin is a dual inhibitor of COX and 5-lipoxygenase (5-LO) with potent anti-inflammatory activity and a favorable gastrointestinal profile.

RIDR-PI-103 is a reactive oxygen species (ROS)-induced drug release prodrug with a self-cyclizing moiety linked to a pan-PI3K inhibitor (PI-103).

L-Ascorbic acid-13C (L-Ascorbate-13C) is the 13C-labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. L-Ascorbic acid exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells.

L-Ascorbic acid-13C6 (L-Ascorbate-13C6) is the 13C-labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. L-Ascorbic acid exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells.

TLR7/8 Antagonist 1 (Compound 16c) is the potent antagonist of TLR7/8 with IC50s of 3.91 and 2.19 μM, respectively. TLR7/8 Antagonist 1 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for treating infectious disease, cancer, and autoimmune disorders.

TLR7/8 antagonist 2 (Compound 15) is a potent and orally active agonist of TLR7/8 with IC50s of 4.9 and 0.6 nM, respectively. Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. TLR7/8 antagonist 2 has the potential for the research of autoimmune diseases.

DB-3-291 is potent and selective CSK degrader, with a Kd of 1 nM.

SM-360320 (CL-087) is a potent, oral actively TLR7 agonist. SM-360320 is a mmuno-modulator and exerts an antitumor effect. SM-360320 can act in synergy with DNA vaccines leading to an enhanced Th1 antibody response. SM-360320 can inhibit HCV replication in hepatocytes via a type I IFN-independent mechanism in addition to its IFN-mediated activity.

TLR7/8 agonist 6 (Compound 4) is the potent agonist of TLR7/8 with IC50s of 0.18 and 5.34 μM, respectively. TLR7/8 agonist 6 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for treating infectious disease, cancer, and autoimmune disorders.

STING agonist-8 is a potent STING agonist with an EC50 of 27 nM in THP1-Dual KI-hSTING-R232 cells (WO2021239068A1, compound 5-AB).

IACS-8779 disodium is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy. IACS-8779 disodium shows robust activation of the STING pathway in vitro and a superior systemic anti-tumor response in the B16 murine model of melanoma.

[D-Leu-4]-OB3 inhibits expressions of pro-inflammatory, proliferative and metastatic genes and PD-L1 expression. [D-Leu-4]-OB3 stimulates expression of pro-apoptotic genes.