Agatolimod (ODN 2006), a class B ODN (oligodeoxynucleotide), is a TLR9 agonist. Agatolimod is also an optimal CpG sequence for humans. Agatolimod stimulates very strong production of NO2 and IL-6 in HD11 cells. Agatolimod can be used for breast cancer research. Sequence: 5'-tcgtcgttttgtcgttttgtcgtt-3'[1][2].
Naphazoline (Naphthazoline) is a potent α-adrenergic receptor agonist. Naphazoline reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF。Naphazoline can be used for non-bacterial conjunctivitis research[1][2].
Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2.
Monophosphoryl lipid A (Glucopyranosyl lipid A) is a toll-like receptor 4 agonist. Monophosphoryl lipid A is derived from the cell wall of nonpathogenic Salmonella. Monophosphoryl lipid A can be used for the research of immunization and vaccine[1].
LMT-28 (LMT28) is a specific blocker of IL-6 signaling via inhibits IL-6Rβ (gp130) with IC50 of 5.9 uM (IL-6–induced luciferase activity), selectively inhibits IL-6–induced phosphorylation of STAT3, JAK2, and gp130; does not affect LIF-induced STAT3 activation and not inhibit IL-11 stimulation on HepG2 cells; binds directly and specifically to gp130, and thereby inhibits the interaction of gp130 with the IL-6/IL-6Rα complex; inhibits IL-6–induced proliferation of the human erythroleukemic cell line TF-1 with IC50 of 7.5 uM; inhibits IL-6–induced TNF-α production, ameliorates the progression of pancreatitis in mice.
ND2158 (ND-2158) is a highly potent and selective IRAK4 inhibitor with IC50 of 1.3 nM;ND2158 demonstrates high selectivity against 334 kinases, and >1000-fold over IRAK1.ND2158 blocked TNF production, collagen-induced arthritis, and gout formation in mice, suppressed LPS-induced TNF production, alleviated collagen-induced arthritis, and blocked gout formation in mouse models.IRAK4 inhibition promoted killing of ABC DLBCL lines harboring MYD88 L265P, by down-modulating survival signals, including NF-κB and autocrine IL-6/IL-10 engagement of the JAK-STAT3 pathway.In ABC DLBCL xenograft models, IRAK4 inhibition suppressed tumor growth as a single agent, and in combination with the Bruton's tyrosine kinase (BTK) inhibitor ibrutinib or the Bcl-2 inhibitor ABT-199.
Denileukin diftitox (DAB 389IL-2) is a diphtheria toxin (DT)-related interleukin 2 (IL-2) fusion protein toxin that depletes cells expressing the high-affinity form of the IL-2 receptor (IL-2R), CD25. Denileukin diftitox binds to cells expressing IL-2R and inhibits protein synthesis through internalization of the diphtheria toxin fragment[1][2][3].
A potent, selective, orally bioavailable IRAK-4 inhibitor that potently inhibits human and rat IRAK-4 activity with subnanomolar order, >30-fold selectivity over IRAK-1; inhibited IL-1β- or TLR ligand lipopolysaccharide (LPS)-induced IL-6 production in human lung alveolar epithelial cells, fibroblast-like synoviocytes, and peripheral blood mononuclear cells; significantly reduces urinary protein excretion and preventd the development of glomerulosclerosis and interstitial fibrosis without affecting the blood pressure in mice model of chronic kidney disease.
Bufrolin is a Cromoglycate (histamine release inhibitor) analog and a high potency agonist of GPR35. Bufrolin promotes interactions between β-arrestin-2 and either human GPR35a or rat GPR35. Bufrolin also serves as antiallergic mast cell stabilizer and inhibit an anti-inflammatory response inducible by the internalization peptide. Bufrolin acts as an anti-inflammatory agent to be used in research of delivering pharmacol linked with internalization peptide[1][2][3].
SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively.
Methoxycoronarin D can be isolated from Hedychium coronarium J. Koenig and is a potent inhibitor of NF-魏B with an IC50 value of 7.3 渭M. Methoxycoronarin D is also a selective inhibitor of COX-1 with an IC50 value of 0.9 渭M[1].
Ivonescimab (AK112) is a PD-1/VEGF Bispecific Antibody. Ivonescimab can be used for cancer research[1][2][3].
Tolfenamic acid-13C6 is the 13C6 labeled Tolfenamic acid. Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity[1].
Salicylic acid-13C6 is the 13C-labeled Salicylic acid (HY-B0167). Salicylic acid is a precursor to and a metabolite of Aspirin (HY-14654), can inhibit cyclo-oxygenase-2 (COX-2) activity[1][2].
Tiaprofenic acid is an orally active nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory and analgesic potency. Tiaprofenic acid inhibits prostaglandin synthesis by suppressing cyclo-oxygenase (COX). Tiaprofenic acid can be used in the treatment of rheumatic diseases[1].
L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist.
Teriflunomide impurity 3 (4-Amino-N-(4-trifluoromethylphenyl)benzamide) is a selective COX-1 inhibitor with an IC50 of 30 µM. Teriflunomide impurity 3 is less active against COX-2 (IC50>100 µM)[1].
COX-2-IN-32 (Compound 2f) is an iNOS and COX-2 inhibitor. COX-2-IN-32 decreases the expression of NF-κB. COX-2-IN-32 has anti-inflammatory activity by inhibits NO production in LPS-induced RAW264.7 macrophages (IC50: 11.2 μM)[1].
Compstatin control peptide is a complement inhibitor.
OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study[1].
JNJ10191584 (VUF6002) maleate (compound 40) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 maleate shows 540-fold selectivity to H4 receptor over the H3 receptor with a Ki value of 14.1 μM. JNJ10191584 maleate inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively[1][2].
Tolmetin sodium is an orally active and potent COX inhibitor with IC50s of 0.35 µM and 0.82 µM human COX-1 and COX-2, respectively. Tolmetin sodium is a non-steroidal anti-inflammatory drug (NSAID)[1][2].
TX-1123 is a potent protein tyrosine kinase (PTK) inhibitor for Src, eEF2-K, and PKA, and EGFR-K/PKC. TX-1123 is a cyclo-oxygenase (COX) inhibitor with IC50 values of 1.16 μM and 15.7 μM for COX2 and COX1, respectively. TX-1123 has low mitochondrial toxicity. TX-1123 can be used in research of cancer[1][2].
TH1020 is a potent and selective toll-like receptor 5 (TLR5)/flagellin complex antagonist with an IC50 of 0.85 μM. TH1020 inhbits flagellin-induced TLR5 signaling. TH1020 is inactive against TLR2, TLR3, TLR4, TLR7 and TLR8[1].
Lib2-1, a macrocyclic peptide, is an IL-17C/IL-17RE interaction inhibitor. Lib2-1 can be used for autoimmune and inflammatory diseases research[1].
PD-1/PD-L1-IN-23 is a potent and orally active inhibitor of PD-1/PD-L1. PD-1/PD-L1-IN-23 is an ester prodrug of L7. L7 is a benzo[c][1,2,5]oxadiazole derivative and biologically evaluated as inhibitors of PD-L1. PD-1/PD-L1-IN-23 displays significant antitumor effects in tumor models of syngeneic and PD-L1 humanized mice[1].
Fidasimtamab (IBI-315; BH2950) is a recombinant human IgG1 bispecific antibody that targets, binds and inhibits both HER2 and PD-1 and their downstream signalling pathways, and links PD-1 expressing T cells to HER2 expressing tumour cells. Fidasimtamab has potential immunosuppressive and antitumor activity[1].
COX-2-IN-27 is a potent and selective COX-2 inhibitor with IC50 values of 13.22, 0.045, 1.67 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-27 shows anti-inflammatory activity[1].
Gumokimab (AK 111) is a monoclonal antibody targeting IL-17A, which can be used in the study of psoriasis, ankylosing spondylitis. Gumokimab competitively blocks the binding of human IL-17A to IL-17R.