Arcapillin is a flavonoid that can be isolated from Artemisia capillaris Thunb. Arcapillin has antispasmodic activity. Arcapillin also has moderate PTP1B inhibitory activity[1][2].
Pep2-8 is a proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor, with an IC50 of 0.8 μM for PCSK9 binding to LDL receptor.
MDL12330A (RMI12330A) is an adenyl cyclase inhibitor. MDL12330A inhibits the vasopressin action on the short-circuit current (SCC). MDL12330A is also an inhibitor of cAMP phosphodiesterase[1].
Izumerogant is an inverse agonist of retinoid-related orphan receptor-gamma (RORγ). Izumerogant (compound 123) also potently inhibits IL-17A, IL-17F and IFN-γ activity with IC50s <50 nM[1][2].
Zofenopril is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 81 μM.
MMP2-IN-3 (compound 2) is a potent MMP-2 (matrix metalloproteinases) inhibitor, with an IC50 of 31 μM. MMP2-IN-3 also shows inhibitory activity against MMP-9 and MMP-8, with IC50 values of 26.6, and 32 μM, respectively[1].
LB-100 is a protein phosphatase 2A (PP2A) inhibitor, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.
Ethacrynic acid (Etacrynic acid sodium) sodium is a diuretic. Ethacrynic acid sodium is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid sodium is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid sodium also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid sodium has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice[1][2][3][4].
16-Hydroxycleroda-3,13-dien-15,16-olide (16ξ-Hydroxycleroda-3,13-dien-15,16-olide; HCD), a clerodane diterpene, is a potent serine protease dipeptidyl peptidase 4 (DPP-4) inhibitor. 16-Hydroxycleroda-3,13-dien-15,16-olide down-regulates LPS-induced ERK phosphorylation in myocyte but blocks GLP-1 induced PKA expression. 16-Hydroxycleroda-3,13-dien-15,16-olide exhibits hypolipidemic, hepatoprotective, hypoglycemic efficacy[1].
PF-06747711 is a potent, selective, and orally active retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) inverse agonist, with an IC50 of 4.1 nM. Anti-skin inflammatory activity[1].
(Rac)-Tanomastat ((Rac)-BAY 12-9566) is the racemate of Tanomastat. Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models[1][2][3].
LmCPB-IN-1 (compound 35) is a potent and reversible covalent Leishmania mexicana cysteine protease B (LmCPB) inhibitor with a pKi of 9.7[1].
Hexylresorcinol is an organic compound with local anaesthetic, antiseptic and anthelmintic properties, is a potent inhibitor of mushroom tyrosinase, causing 90% loss of activity at 100 μM.
Chymotrypsin (Chymotrypsin A) is a serine protease produced by the pancreas. Chymotrypsin cleaves protein chains at the carboxyl side of aromatic amino acids[1][2].
Spirapril is a potent and cross the blood-brain barrier angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active prodrug of Spiraprilat and can be used for the research of hypertension, congestive heart failure[1][2][3].
Manoalide is a potent Phospholipase A2 (PLA2) and Phospholipase C (PLC) inhibitor. Manoalide, a sesterpenoid compound, displays anti-inflammatory and antibacterial activities[1][2][3].
ATX inhibitor 20 (compound 24) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.3 nM[1].
Nampt-IN-5 is a potent and orally active nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively[1].
hACC2-IN-1 is a potent acetyl-CoA carboxylase 2 (ACC2) inhibitor, with an IC50 value of 2.5 μM (hACC2). hACC2-IN-1 could be used for obesity research[1].
KC7F2 is a potent HIF-1 pathway inhibitor and that its potential as a cancer therapy agent warrants further study.Target：HIFin vitro: KC7F2 is the second HIF-1α inhibitor. KC7F2 is shown to inhibit the proliferation of cancer cells, an effect that is increased in hypoxia, while non-tumor cells are less sensitive. KC7F2 decreases HIF-1α levels by downregulating HIF-1α protein synthesis. [2] KC7F2 markedly inhibits HIF-mediated transcription in cells derived from different tumor types, including glioma, breast and prostate cancers and exhibited enhanced cytotoxicity under hypoxia. KC7F2 prevents the activation of HIF-target genes such as Carbonic Anhydrase IX, Matrix Metalloproteinase 2 (MMP2), Endothelin 1 and Enolase 1. KC7F2 works through the down-regulation of HIF-1α protein synthesis, an effect accompanied by the suppression of the phosphorylation of eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and p70 S6 kinase (S6K), key regulators of HIF-1α protein synthesis.[1]
MY-5445 is a specific phosphodiesterase type 5 (PDE5) inhibitor[1].
CMI977 is a potent 5-Lipoxygenase (5-LO) inhibitor.
IDO5L is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 67 nM.
PQ-10 is a potent inhibitor of Phosphodiesterase 10A (PDE10A) with IC50 andED50 of 4.6 nM and 13 mg/kg, respectively. PQ-10 induces patterns of brain glucose metabolism which can be a potential translational biomarker. PQ-10 has the potential for researching psychiatric disorders like schizophrenia[1].
Sacubitril sodium is a potent and orally active NEP (neprilysin) inhibitor, with an IC50 of 5 nM. Sacubitril sodium enhances the tone of the natriuretic peptide (NP) system and exerts significant antihypertensive effects. Sacubitril sodium is a component of the heart failure medicine LCZ696. Sacubitril sodium can be used for the research of heart failure, hypertension and COVID-19[1][2][3].
Flavoxate is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate can be used for the research of overactive bladder (OAB) and lower urinary tract infections[1][2].
PYR-41 is a specific and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with no or little activity at E2.
Dabigatran-d4 is deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
5-O-Methylembelin is a natural isocoumarin that inhibits PCSK9, low-density lipoprotein receptor (IDOL), and sterol regulatory element binding protein 2 (SREBP2) mRNA expression[1].
Serotonin hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.