Irsenontrine (E2027) is an orally active and selective phosphodiesterase 9 (PDE 9) inhibitor. Irsenontrine can be used for the research of neurological diseases[1].
Fraxamoside is a competitive xanthine oxidase inhibitor with an IC50 of 16.1 μM and a Ki of 0.9 μM[1].
Sitagliptin-d4 (MK-0431-d4) phosphate is the deuterium labeled Sitagliptin phosphate. Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[1][2].
Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer treatment.
Alogliptin benzoate(SYR 322) is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9.IC50 value: <10 nMTarget: DPP4Alogliptin is an orally administered, anti-diabetic drug in the DPP-4 inhibitor class. A randomized clinical trial reporting in 2011 aimed to determine the efficacy and safety of alogliptin versus placebo and voglibose among newly diagnosed Type 2 diabetes patients in Japan. The main outcome indicated that alogliptin was statistically superior to both comparitors. A randomized clinical trial reporting in 2012 aimed to demonstrate that alogliptin was "non-inferior" to a "very low fat/calorie traditional Japanese diet" among newly diagnosed Type 2 diabetes patients in Japan. The outcome indicated that both the drug and dietary treatments comparably impacted indicators of the diabetic condition, such as HbA1c levels and glycemic efficacy. The drug treatment had its impact without changing body mass index (BMI), but the dietary treatment was accompanied by a significant reduction in the BMI…
Picrinine, an akuammiline alkaloid, is isolated from the leaves of Alstonia scholaris. Picrinine exhibits anti-inflammatory activity through inhibition of the 5-lipoxygenase enzyme[1].
Nelfinavir-d3 (AG1341-d3) is the deuterium labeled Nelfinavir. Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent[1][2][3].
PSN-GK1 is a potent glucokinase activator with an EC50 of 0.13 μM.
GS-9256 is a selective HCV NS3 protease inhibitor. GS-9256 has good pharmacokinetic properties and antiviral activity[1].
Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule[1].
SHP394 is an orally efficacious protein tyrosine phosphatase SHP2 inhibitor with an IC50 of 23 nM[1].
DHODH-IN-14 (Compound 7l) is a hydroxyfurazan analog of A771726. DHODH-IN-14 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 0.49 μM for rat liver DHODH. DHODH-IN-14 can be used for rheumatoid arthritis[1].
Olivetol-d9 is the deuterium labeled Olivetol. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2[3]. Olivetol also inhibits CYP2C19 and CYP2D6 activi
Ethyl 3,4-dihydroxybenzoate (Ethyl protocatechuate), an antioxidant, is a prolyl-hydroxylase inhibitor found in the testa of peanut seeds. Ethyl 3,4-dihydroxybenzoate protects myocardium by activating NO synthase and generating mitochondrial ROS. Ethyl 3,4-dihydroxybenzoate induces cell autophagy and apoptosis in ESCC cells. Ethyl 3,4-dihydroxybenzoate is a collagen synthesis inhibitor and has a bone protecting-effect[1][2][3][4].
Novobiocin (Albamycin) is a potent and orally active antibiotic. Novobiocin also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin shows anti-orthopoxvirus activity[1][2][3][4][6].
MMP-2/MMP-9-IN-1 is a highly selective, orally active and potent type IV collagenase (MMP-9 and MMP-2) inhibitor with IC50s of 0.24 and 0.31 μM for MMP-9 and MMP-2, respectively. MMP-2/MMP-9-IN-1 is orally active in animal models of tumor growth and metastasis. MMP-2/MMP-9-IN-1 can be used for the research of cancer[1].
MeDTC (S-Methyl-N,N-diethylthiocarbamate Sulfone), a Disulfiram metabolite, is a potent, irreversible aldehyde dehydrogenase (ALDH) inhibitor[1].
ATX inhibitor 8 is a Autotaxin (ATX) inhibitor extracted from patent WO2018212534A1 compound 96[1].
Saikogenin A, extracted from a Chinese herbal plant called Tsai-Fu, is a dipeptidyl peptidase-IV (DPP-IV) inhibitor.
Otaplimastat (SP-8203), a matrix metalloproteinase (MMP) inhibitor, blocks N-methyl-D-aspartate (NMDA) receptor-mediated excitotoxicity in a competitive manner. Otaplimastat also exhibits anti-oxidant activity. Otaplimastat can be used for the research of brain ischemic injury[1][2][3].
Atovaquone (4-chlorophenyl-2,3,5,6-d4) is the deuterium labeled Atovaquone. Atovaquone is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome bc1 complex. Atovaquone is against human and P. falciparum cytochrome bc1 activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia[1][2].
Talabostat mesylate is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM.
1-Ethynylpyrene is an aryl acetylenic inhibitor of cytochromes P450 1A1, 1A2, and 2B1 with IC50s of 0.18, 0.32, and 0.04 μM, respectively[1].
SR 42128 is a potent renin inhibitor. SR 42128 potently inhibits primate renins whereas other animal renins are much less inhibited[1].
Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect[1][2][3][4][5][6][7].
DPM-1001 is a potent, specific, orally bioavailable and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM, an an analog of the specific PTP1B inhibitor trodusquemine (MSI-1436; IC50=600 nM). DPM-1001 has anti-diabetic property[1].
Ongericimab (JS002) is a humanized anti-PCSK9 monoclonal antibody. Ongericimab has lipid-lowering efficacy. Ongericimab can be used in research of hypercholesteremia and hyperlipidemia[1].
Ala-Ala-Pro-Val-chloromethylketone is an irreversible human neutrophil elastase (NE) inhibitor for use in the study of chronic inflammatory airway diseases[1].
FKGK18 (FKGK18) is a potent, selective inhibitor of iPLA2 (group VIA Ca2+-independent phospholipase A2) with IC50 of 50 nM; displays 195 and >455 times more potent for GVIA iPLA(2) than for GIVA cPLA(2) and GV sPLA(2); inhibits Ca2+-independent PLA2 activity in a concentration-dependent manner, similar to S-BEL, which preferentially inhibits cytosol-associated iPLA2β; FKGK18 a valuable tool to explore the role of GVIA iPLA(2) in cells and in vivo models.
TNO155 is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). TNO155 has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors[1].