NAAA-IN-3 (Compound 17a) is a potent and selective inhibitor of NAAA with an IC50 of 50 nM. NAAA is a cysteine amidase which preferentially hydrolyzes the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). NAAA-IN-3 has the potential for the research of inflammation and pain[1].
Crocetin (β-Crocetin), isolated from Crocus sativus, possesses anti-inflammatory, neuroprotective and antioxidant activity[1][2].
Ascochlorin (Ilicicolin D), an isoprenoid antibiotic, mediates its anti-tumor effects predominantly through the suppression of STAT3 signaling cascade. Ascochlorin induces apoptosis. Anti-inflammatory activity[1][2][3].
Cyclosporin D, a metabolite of Cyclosporin A, is a weak immunosuppressant. Cyclosporin D is used as internal standard for quantification of Cyclosporin A[1][2]. Cyclosporin A is a potent immunosuppressant drug, suppress T cell activation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activated T cells (NFAc)[3].
Tacrolimus monohydrate binds to FK506 binding protein (FKBP). This complex inhibits calcineurin phosphatase (PP2B). Tacrolimus monohydrate is a mTOR-independent autophagy inducer.
EM 163 is a TIR-TIR interaction inhibitor, which is a TIR (Toll/interleukin-1 receptor) structural domain mimic of the MyD88 protein. EM 163 targets the TIR structural domain in the IL-1 receptor and blocks the interaction with MyD88. EM 163 inhibits the production of inflammatory cytokines in vivo caused by staphylococcal enterotoxin B (SEB). EM 163 protects mice from SEB shock-induced death. In rat hippocampal neurons in vitro, EM 163 blocked the activation of p38 and the inhibitory effect of IL-1β on chemically induced long-term potentiation (LTP)-triggered protein synthesis.
Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention[1][2][3][4].
Ecubectedin is a derivative. Ecteinascidins is a family of tetrahydroisoquinoline alkaloids with wide range of antitumor and antimicrobial activities[1].
Hydrocortisone hemisuccinate (Hydrocortisone 21-hemisuccinate), a physiological glucocorticoid, and is an orally active steroidal anti-inflammatory drug (SAID). Hydrocortisone hemisuccinate inhibits proinflammatory cytokine activity, with IC50s of 6.7 and 21.4 μM for IL-6 and IL-3, respectively. Hydrocortisone hemisuccinate can be used for the research of ulcerative colitis (UC)[1][2][3].
Rabeprazole D4 (LY307640 D4) is a deuterium labeled Rabeprazole. Rabeprazole is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux[1][2][3].
Anthraquinone-2-carboxylic acid is a major anthraquinone isolated from Brazilian taheebo, with anti-inflammatory activity and antinociceptive[1].
Mal-amido-PEG8-acid (example 143) is an ADC linker, extracted from patent US2018339985[1].
Antipyrine is an analgesic and antipyretic agent.Target: OthersAntipyrine is an analgesic and antipyretic that has been given by mouth and as ear drops. Antipyrine is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. Antipyrine was one of the first important synthetic drugs. antipyrine went into widespread clinical use as an antipyretic the same year it was synthesized. Two years after its introduction, reports began to appear of its analgesic effects and in the succeeding years, as the use of antipyrine as an antipyretic declined, it gained considerable popularity as an analgesic. The plasma halflife of antipyrine is significantly longer and the clearance significantly lower in the elderly group. This finding of an impaired metabolism of antipyrine in the elderly has since been confirmed in a much larger study and subsequently other drugs have been shown to be metabolized more slowly in this age group [1].
DGKα-IN-3 (example 25) is a DGKα inhibitor with the IC50 of 283 nM, extracted from patent WO2021105115. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-2 has the potential for cancer and immunology study.
Perphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), .6 nM (5-HT2A), respectively. Perphenazine dihydrochloride also binds to Alpha-1A adrenergic receptor. Perphenazine dihydrochloride inhibits cancer cell proliferation, and induces apoptosis. Perphenazine dihydrochloride can be used in the research of mental disease, cancer, inflammation[1][3][5].
Glycolithocholic acid, an endogenous metabolite, is a glycine-conjugated secondary bile acid. Glycolithocholic acid can be used to diagnose ulcerative colitis (UC), non-alcoholic steatohepatitis (NASH) and primary sclerosing cholangitis (PSC)[1][2][3][4].
L 888607 Racemate is a selective prostaglandin D2 receptor subtype 1 (DP1) antagonist, with Kis of 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively.
4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties[1][2].
MIF-IN-6 (compound 2d) is a potent macrophage migration inhibitory factor (MIF) inhibitor with an IC50 of 1.4 μM and a Ki value of 0.96 μM, respectively. MIF-IN-6 attenuates MIF-induced ERK phosphorylation and inhibits proliferation of A549 cells[1].
Vamikibart is a chimeric humanized IgG2κ antibody targeting IL6[1].
FXR agonist 5 (compound 1) is a FXR agonist. FXR agonist 5 can be used for research in diseases or disorders caused by metabolic inflammation[1].
9-Hydroxycanthin-6-one is an alkaloid compound. 9,10-Dimethoxycanthin-6-one exhibits NF-κB inhibitory effects with an IC50 of 3.8 μM[1].
Triflusal-d3 is deuterium labeled Triflusal.
Naproxcinod (Nitronaproxen) is the first in class of cyclooxygenase (COX)-inhibiting nitric oxide donators (CINODs). Naproxcinod shows analgesic and anti-inflammatory effects, it can be used for the research of osteoarthritis and inflammation[1][2][3].
Evogliptin tartrate is a potent, orally bioavailable and selective dipeptidyl peptidase-4 (DPP-4) inhibitor, with antidiabetic activity. Evogliptin tartrate has potential for anti-atherosclerosis therapy that targets arterial inflammation[1].
Sedanolide, a natural compound occurring in edible umbelliferous plants, possesses anti-inflammatory and antioxidant activities[1][2].
Moracin P is a 2-arylbenzofuran isolated from the Mori Cortex Radicis. Moracin P exhibits potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1). Moracin P reduces oxygen-glucose deprivation (OGD)-induced reactive oxygen species (ROS) production. Moracin P has neuroprotective and anti-inflammatory effects[1][2][3].
Pegbelfermin (BMS-986036) is a polyethylene glycol-modified (PEGylated) analogue of human fibroblast growth factor 21 (FGF21). Pegbelfermin can be used for the research of nonalcoholic steatohepatitis (NASH)[1][2].
Nogapendekin alfa is a superagonist of IL-15. Nogapendekin alfa promotes the proliferation and viability of immune cells. Nogapendekin alfa combines with Inbakicept (HY-P99661) at a ratio of 2:1, to form ALT-803, an IL-15 cytokine antibody fusion protein. ALT-803 reduces tumor burden by activation of NK cells and CD8+ T cells[1].
BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP[1].