Alkannin, found in Alkanna tinctoria, is used as a food coloring. Alkannin shows anticancer activity, arrests cell cycle, and induces apoptosis. Alkannin improves hepatic inflammation in a Rho-kinase pathway[1][2][3].
Bisoprolol fumarate is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol fumarate has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research[1][2].
Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent[1].
Vemircopan is a complement factor D inhibitor[1].
Roflupram is a selective, orally active and brain-penetrant PDE4 inhibitor, with an IC50 of 26.2 nM for core catalytic domains of human PDE4. Roflupram can reverse cognitive deficits and reduce the production of pro-inflammatory factors[1][2].
Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
C5aR-IN-3 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-3 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 89)[1].
Sephin 1 (NSC 65390) is a selective inhibitor of PPP1R15A that disrupts the PPP1R15A-PP1c complex but spares the related PPP1R15B-PP1c complex; prolongs eIF2α phosphorylation after stress, attenuates the expression of stress genes such as CHOP, and protects cells from cytotoxic ER stress; lacks any measurable α2-adrenergic agonist activity in a cell-based assay, in contrast to Guanabenz; safely prevents the motor, morphological, and molecular defects in mice.
Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively[2]. Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment[5].
AMT hydrochloride is a selective inhibitor of inducible NOS (iNOS) with Ki of 4.2 nM[1].
25S-Inokosterone is a phytoecdysone in the roots of two same species of A. bidentata Blume and A. japonica Nakai, and two different species of C. capitata Moq and C. officinalis Kuan. 25S-Inokosterone has the potential for the LPS-induced acute kidney injury research[1][2].
PIT (2,2'-Pyridylisatogen tosylate) is a selective and non-competitive antagonist of P2Y1 receptor with an IC50 value of 0.14 μM for human P2Y1 receptor. PIT antagonizes P2Y1 receptor signaling without affecting nucleotide binding. PIT is an irreversible antagonist of responses to ATP at metabotropic purinoceptors (of the P2Y family) in some smooth muscles. PIT can be used for the research of chronic bronchitis and asthma[1][2][3].
Dulcioic acid (compound 19) is a product isolated from Tripterygium wilfordii Hook f. Dulcioic acid shows a significant inhibitory effect on cytokine production[1].
UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC50 of 11 nM, selective over PI3KC2 α, β, and γ lipid kinases. UCB9608 improves metabolic stability and exhibits excellent pharmacokinetic profile, acts as a potent immunosuppressive agent[1].
m-PEG6-azide is a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
Anemarrhenasaponin Ia, isolated from Anemarrhenae rhizome, inhibits N-formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide generation. Anemarrhenasaponin Ia is an useful anti-inflammation reagent[1].
MEK-IN-4 is a MEK inhibitor. MEK-IN-4 can be used for the research of inflammatory disorders and cancers[1].
J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats[1][2].
Sucralfate is a cytoprotective agent which has been employed for prevention and treatment of several gastrointestinal diseases.
Salmeterol xinafoate is a long-acting beta-2 adrenergic receptor (β2AR) agonist, with Ki of 1.5 nM for WT β2AR, and used for asthma treatment.
Belimumab (LymphoStat B) is a human IgG1λ monoclonal antibody that inhibits B-cell activating factor (BAFF). Belimumab can be used for systemic lupus erythematosus (SLE) research[1].
Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist that is widely used as an immunosuppressant and chemotherapeutic agent[1].
Citroside A is a megastigmane sesquiterpenoid with cytotoxic and anti-inflammatory activities. Citroside A displays potential effects against NO production with an IC50 of 34.25 μM. Citroside A exhibits pronounced cytotoxicity against SGC-7901 and HeLa cells with IC50 values of 27.52 μM and 29.51 μM, respectively[1].
Hispolon, a polyphenol, can be isolated from Phellinus linteus. Hispolon possesses anticancer, antidiabetic, antioxidant, antiviral, hepatoprotective, anti-diabetic, and anti-inflammatory activities[1].
L-Alanyl-L-glutamine, a glutamine dipeptide, is benefit for the antioxidant system, attenuating inflammation, and may modulate the heat shock protein (HSP) response in catabolic situations[1].
Hosenkoside F is a baccharane glycoside isolated from the seeds of impatiens balsamina.
4-Hydroxyretinoic acid (4-HRA) is a naturally occurring retinoid derivative with diverse biological effects. 4-Hydroxyretinoic acid is formed from retinol catalyzed by cytochrome P-450 isozyme(s), and is mainly metabolized by the liver in the body. 4-Hydroxyretinoic acid also serves as the substrate for human liver microsomal UDP-glucuronosyltransferase(s) and recombinant UGT2B7. 4-Hydroxyretinoic acid regulates gene expression and cell differentiation via binding to nuclear receptor RAR (Retinoic Acid Receptor), and activates RARs and RXR-alpha, to induce cancer cell apoptosis. In addition, 4-Hydroxyretinoic acid is also involved in various physiological processes such as immune regulation, neuroprotection, and anti-oxidation[1][2].
(S)-(-)-Propranolol hydrochloride is a β-adrenergic receptor antagonist with log Kd values of -8.16, -9.08, and -6.93 for β1, β2, and β3, respectively. (S)-(-)-Propranolol hydrochloride the active enantiomer of propranolol and can be s used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[2].
Kadsulignan N, a natural product has anti-HIV activity (EC50: 43.56 μM). Kadsulignan N is also a COX-2 ligand (Ki: 72.24 nM)[1][2].
Tris(2,4-di-tert-butylphenyl)phosphate is an active compound from the leaves of Vitex negundo L. shows anti-inflammatory activity with evidence of inhibition for secretory Phospholipase A2 (sPLA2) through molecular docking[1].