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].
Phenethyl ferulate is a major constituent ofQianghuo, shows inhibitory activity against cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) with IC50 values of 4.35 μM and 5.75 μM, respectively[1].
TCS 401 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B).
SA57 is a potent, selective FAAH inhibitor with IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC50s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC50 of 850 nM), but not other brain serine hydrolases[1][2].
PD 113413 is formed by subsequent hydrolysis of the diketopiperazine quinapril analog. PD 113413 is a potent angiotensin-converting enzyme inhibitor. PD 113413 can be used for research of hypertension and congestive heart failure[1].
Lodelaben is a human neutrophil elastase inhibitor with an IC50 and Ki of 0.5 and 1.5 μM, respectively.
PDEδ-IN-99 is a novel potent K-Ras-PDEδ inhibitor that binds to the farnesyl binding pocket of PDEδ with Kd of 8±4 nM.
Cornoside is a phenolic glycoside and has inhibitory effect on rat lens aldose reductase (AR) with an IC50 of 150 μM[1].
ε-Viniferin, the dimer of Resveratrol and isolated from Vitis vinifera, displays a potent inhibitory for all the CYP activities, with Ki values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant capacity[1][2].
9-cis-Retinoic acid-d5 (ALRT1057-d5) is the deuterium labeled 9-cis-Retinoic acid. 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities[1][2][3][4][5][6].
Enazadrem is a 5-lipoxygenase inhibitor with antiinflammatory activities.
Opicapone is an available catechol-O-methyltransferase (COMT) inhibitor. Opicapone decreases the ATP content of the cells with IC50 values of 98 μM.
NUCC-0223619 is an IDO1 inhibitor, induce degradation of IDO protein. NUCC-0223619 can be used to synthesis PROTAC[1].
Omesdafexor is a FXR agonist. Omesdafexor can be used in the research of liver disease or a metabolic inflammation-mediated disease[1][2].
Ranirestat (AS-3201) is an aldose reductase inhibitor being developed for the treatment of diabetic neuropathy.
Lisinopril is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.Target: ACELisinopril is a potent, competitive inhibitor of angiotensin-converting enzyme (ACE), the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Lisinopril may be used to treat hypertension and symptomatic congestive heart failure, to improve survival in certain individuals following myocardial infarction, and to prevent progression of renal disease in hypertensive patients with diabetes mellitus and microalbuminuria or overt nephropathy [1, 2].
PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development[1].
FR 901537 is a potent and competitive aromatase inhibitor. FR 901537, a novel naphthol derivative, has the potential for breast cancer research[1].
Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP), including PP1 (IC50=15-50 nM), PP2A (IC50=0.1-0.3 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), with a significantly higher affinity for PP2A. Okadaic acid increase of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter[1] [2].
(Rac)-Nutlin-3 (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). (Rac)-Nutlin-3 inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. (Rac)-Nutlin-3 has the potential for the study of TP53 wild-type ovarian carcinomas[1][2].
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity[1][2].
WES-1 (Compound 8g) is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). WES-1 has broad spectrum anti-proliferative activity against the cancer cells, such as leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI–H460), colon cancer (HCT 116 and HCT-15) and melanoma (LOX IMVI) cell lines[1].
IDO-IN-18 (Compound 00815) is an IDO inhibitor. IDO-IN-18 can be used for research of immunosuppression associated infectious or cancer diseases[1].
Razuprotafib is a potent protein tyrosine phosphatase β (HPTPβ) inhibitor.
Fosfenopril is a potent angiotensin converting enzyme (ACE) inhibitor. Fosfenopril alleviates lipopolysaccharide (LPS)-induced inflammation by inhibiting TLR4/NF-κB signaling in monocytes[1][2].
Enteropeptidase (TMPRSS15), a type II transmembrane serine protease and a physiological activator of trypsinogen. Enteropeptidase is associated with the brush border membrane (BBM) of the enterocytes in the upper small intestine. Trypsinogen is the primary substrate for Enteropeptidase. Enteropeptidase is involved in digestion in humans and animals[1].
Elastatinal is a potent and competitive inhibitor of elastase, with a Ki of 0.21 μM. Elastatinal more potently inhibits pancreatic elastase versus leucocyte elastase. Elastatinal shows no activity on human leucocyte chymotrypsin-like protease[1][2][3][4].
MMP-7-IN-3 is a potent and selective inhibitor of MMP-7. MMP-7-IN-3 suppresses kidney fibrosis progression in a mouse model with unilateral ureteral obstruction[1].
Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice[1].
D-Isofloridoside, one of the polysaccharide precursors, has the activity of scavenging free radicals, inhibiting ROS expression, and inhibiting MMP-2 and MMP-9[1][2].