Hydroxyevodiamine (Rhetsinine) inhibits aldose reductase with an IC50 value of 24.1 μM[1].
ER-50891 is a potent antagonist of retinoic acid receptor α(RARα). ER-50891 significantly attenuates ATRA's inhibitive effects on BMP 2-induced osteoblastogenesis[1].
hCAIX/XII-IN-2 (compound 6a) is a potent and selective hCAIX and hCAXIIinhibitor with Ki values of >10000, >10000, 30.0, 3.6 nM for hCAI, hCAII, hCAIX and hCAXII, respectively[1].
Trandolaprilate hydrate is a potent angiotensin-converting enzyme (ACE) inhibitor. Trandolaprilate hydrate partially inhibits angiotensin-I-mediated c-fos induction. Trandolaprilate is main bioactive metabolite of Trandolapril. Trandolaprilate shows high lipophilicity[1][2].
K579 is a potent and orally active dipeptidyl peptidase IV inhibitor. K579 inhibits the blood glucose elevation. K579 increases the plasma insulin and active forms of glucagon-like peptide-1 (GLP-1). K579 has the potential for the research of diabetic[1].
Metyrapone is an inhibitor of cytochrome P450-mediated ω/ω-1 hydroxylase activity and CYP11B1.Target: CYP11B1Metyrapone is a drug used in the diagnosis of adrenal insufficiency and occasionally in the treatment of Cushing's syndrome (hypercortisolism). Metyrapone blocks cortisol synthesis by reversibly inhibiting steroid 11β-hydroxylase. This stimulates ACTH secretion, which in turn increases plasma 11-Deoxycortisol levels.
BIIB021 is an orally available, fully synthetic inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively.
Trimyristin, an active molluscicidal component of Myristica fragrans Houtt, significantly inhibits acetylcholinesterase (AChE), acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata. IC50s of Trimyristin against AChE, ACP, and ALP are 0.11, 0.16 and 0.18 mM, respectively[1].
Anticancer agent 143 (compound 369) is a dual PTPN2/PTP1B inhibitor with IC50 values <2.5 nM. Anticancer agent 143 can be used in cancer research[1].
Olprinone(Loprinone) is a selective phosphodiesterase 3 (PDE3) inhibitor. IC50 value:Target: PDE3Olprinone is used as cardiotonic agent with positive inotropic and vasodilating effects. Olprinone has been reported to improve microcirculation and attenuate inflammation. Olprinone is often used to increase cardiac output after cardiopulmonary bypass (CPB). Olprinone was infused at a rate of 0.2 μg/kg/min when weaning from CPB was started. Olprinone has also shown potent antioxidative and anti-inflammatory effects in the meconium-induced oxidative lung injury.
SDZ-MKS 492 (MKS 492) is a selective type III isozyme inhibitor of cyclic nucleotide phosphodiesterase, effective in allergic bronchoconstriction and platelet activating factor (PAF) or LTB4-induced inflammatory reactions in animals[1].
DHODH-IN-3 (compound 3) is a potent inhibitor of Human Dihydroorotate Dehydrogenases (HsDHODH) with an IC50 value of 261 nM. DHODH-IN-3 binds to the the ubiquinone binding cavities in DHODH with a Kiapp of 32 nM. DHODH-IN-3 has the potential for malaria treatment[1].
Isoglycycoumarin is a flavonoid isolated from the roots of Glycyrrhiza uralensis. Isoglycycoumarin is a highly selective probe for human cytochrome P450 2A6 (CYP2A6)[1][2].
JE-2147 (AG1776) is a potent dipeptide protease inhibitor with a Ki of 0.33 nM for HIV-1 protease. JE-2147 has effective activities against a wide spectrum of HIV-1, HIV-2, simian immunodeficiency virus, and various clinical HIV-1 strains in vitro[1][2].
PTP1B-IN-8 is a potent and selective potent protein tyrosine phosphatase-1B (PTP1B) inhibitor extracted from patent CN103626692A, example 1[1].
Aloin (mixture of A&B) is anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) has diverse biological activities such as anti-inflammatory, immunity, antidiabetic, antioxidant, antibacterial, antifungal, and antitumor activities. Aloin (mixture of A&B) also an effective inhibitor of stimulated granulocyte matrix metalloproteinases (MMPs)[1][2].
Morin 3-O-β-D-glucopyranoside is a natural flavonoid with antifungal, anticancer and antioxidant activities. Morin 3-O-β-D-glucopyranoside inhibits reverse transcriptase, protein-tyrosine kinase and xanthine oxidase, and also shows anti-HIV, antiarteriosclerotic, and superoxide scavenging activities[1].
TM5441 is a plasminogen activator inhibitor-1 (PAI-1); inhibits several tumor cell lines with IC50 values between 9.7 and 60.3 μM.
Aminopeptidase-IN-1 (compound 16o) is a potent insulin-regulated aminopeptidase (IRAP) inhibitor with an Ki value of 7.7 μM. Aminopeptidase-IN-1 can be used tor research cognitive and memory impairments[1].
PFKFB3-IN-2 is a 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) inhibitor. PFKFB3-IN-2 has potential applications in cancer, neurodegenerative diseases, autoimmune diseases, inflammatory diseases, multiple sclerosis, metabolic diseases, angiogenesis inhibition and other diseases[1].
PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration[1].
PF-03049423 is a potent, selective, orally active, and brain penetrant inhibitor of PDE5 with IC50 of 0.2 nM; displays 158-fold and 2460-fold selectivity over PDE6 and PDE11, respectively; possesses an excellent potency and selectivity profile and demonstrates robust in vivo blood pressure lowering in a spontaneously hypertensive rat (SHR) model. Stroke Phase 2 Discontinued
H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. H-Tyr-Phe-OH can be used as an biomarker for differentiating benign thyroid nodules (BTN) from thyroid cancer (TC). H-Tyr-Phe-OH exhibits xanthine oxidase inhibition (uric acid lowering) activity and serves as regulator in IL-8 production in neutrophil-like cells[1][2][3][4].
Cordycepin, which is a nucleoside derivative isolated from Cordyceps, inhibits IL-1β-induced MMP-1 and MMP-3 expression in rheumatoid arthritis synovial fibroblasts (RASFs) in a dose-dependent manner.
Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator.
DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
Bezeparsen is a PCSK9 synthesis inhibitor[1].
GW280264X is the mixed ADAM10/TACE (ADAM17) metalloproteinases inhibitor. GW280264X potently blocks TACE (ADAM17) and ADAM10 with IC50s of 8.0 nM and 11.5 nM, respectively[1]. ADAM10 and 17 modulate the immunogenicity of glioblastoma-initiating cells[2].
Atorvastatin hemicalcium trihydrate is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin hemicalcium trihydrate inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively[1][2][3].
MMP145 (compound 27) is a potent, selective and orally active MMP-12 inhibitor. MMP145 is effective in inflammation and asthma reasearch[1].