AR7 is a retinoic acid receptor α (RARα) antagonist.
5-Amino-8-hydroxyquinoline (5A8HQ), a potential anticancer candidate, has promising proteasome inhibitory activity.
(R)-6',7'-Dihydroxybergamottin ((R)-6′,7′-DHB) is a competitive inhibitor of human and rat CYP1A1 activity with Kis of 55 μM and 1.72 μM, respectively. (R)-6',7'-Dihydroxybergamottin has the potential for cancer research[1].
Sevelamer is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
LHVS is a potent, non-selective cysteine protease inhibitor[1]. LHVS effectively blocks T. gondii microneme protein secretion (IC50=10 μM), gliding motility, and cell invasion[2].
PRL-3 Inhibitor I is a potent PRL-3 inhibitor with an IC50 of 0.9 μM. PRL-3 Inhibitor I shows a reduced invasion in cell-based assay[1].
FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect[1][2].
RORγt modulator 3 (Compound 23) is a modulator of retinoid-related orphan receptor γt (RORγt). RORγt modulator 3 can be used for the research of RORyt mediated diseases such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer[1].
Leptosin D, a thiodiketopiperazine alkaloid, is a mushroom tyrosinase inhibitor, with an IC50 of 28.4 μM[1].
6,7-Dihydroxy-4-coumarinylacetic acid is a potent and selective inhibitor of ALR2. 6,7-Dihydroxy-4-coumarinylacetic acid inhibits ALR2, SDH andALR1 with IC50s of 9.6, 288 and 66.3 μM, respectively. 6,7-Dihydroxy-4-coumarinylacetic acid clearly suppresses galactitol accumulation[1].
Nanterinone (UK 61260) is a positive inotropic and arterial vasodilating agent. Nanterinone is a phosphodiesterase inhibitor[1].
Compounds 6B and 14g showed significant inhibitory effect on tumor related subtype HCA IX with low nanomolar potency, while 6K was effective on HCA XII. Compounds 6B, 14g and 6K can be considered as the leading molecules for the development of future cancer therapeutic drugs based on new mechanisms of action.
Evogliptin (DA-1229) is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation[1][2][3][4].
Salicylanilide demonstrates a wide range of biological activities including antiviral potency which can inhibit HIV virus by targeting HIV-1 integrase or reverse transcriptase.
Olumacostat glasaretil is a small molecule inhibitor of acetyl coenzyme A carboxylase (ACC).
Calpain-2-IN-1 is a calpain-2 selective inhibitor that enhances learning & memory by prolonging ERK activation.
DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration[1].
Sitagliptin is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts.
Dencichin is a non-protein amino acid originally extracted from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 (PHD-2) activity.
Etesevimab (JS016) is a recombinant neutralizing human IgG1 anti-SARS-CoV-2 monoclonal antibody[1].
Rosamultin is a 19 α-hydroxyursane-type triterpenoid isolated from Potentilla anserina L. Rosamultin has inhibitory effects against HIV-1 protease[1]. Rosamultin has the potential for treating H2O2-induced oxidative stress injury through its antioxidant and antiapoptosis effects[2].
Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases (extracted from patent WO2011057115A1 and WO2011057121A1)[1][1].
H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH is a water-soluble polypeptide that can serve as a substrate for cathepsin D, pepsin and pepsinogen. H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH has potential applications in biochemical analysis[1][2].
Flazin is a non-enzymatic protein glycation inhibitor, also inhibits peroxynitrite (ONOO-), with an IC50 value of 85.31 μM for bovine serum albumin (BSA) glycation and an EC50 value of 71.99 μM for ONOO-. Flazin can be used for researching diabetes and neuronal disorders. Flazin also can used as a lipid droplet (LD) regulator against lipid disorders, and a xanthine oxidase (XOD) inhibitor[1][2][3].
N-Benzyllinolenamide is a natural macamide isolated from Lepidium meyenii, acts as an inhibitor of fatty acid amide hydrolase (FAAH) with an IC50 of 41.8 μM[1].
HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway[1].
DHODH-IN-15 (Compound 7b) is a hydroxyfurazan analog of A771726. DHODH-IN-15 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 11 μM for rat liver DHODH. DHODH-IN-15 can be used for rheumatoid arthritis[1].
Arimoclomol (BRX-220 free base) is a co-inducer of heat shock proteins (HSP).
2-Ketoglutaric acid-d4 is the deuterium labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
TAT-cyclo-CLLFVY is a selective HIF-1 dimerization inhibitor. TAT-cyclo-CLLFVY blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50=1.3 μM). TAT-cyclo-CLLFVY inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cancer cells in vitro. TAT-cyclo-CLLFVY also reduces tubularization of hypoxic HUVECs.