Simvastatin acid (Tenivastatin) is an orally active HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid can reduce cholesterol synthesis and lower blood cholesterol levels[1]. Simvastatin acid shows anti-proliferation activities against cancer cells and induces apoptosis[2].
DG051 is a potent leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis in the enzyme assay with an IC50=47 nM.
SCD inhibitor 1 is a stearoyl-coa desaturase (SCD) extracted from patent WO/2009060053 A1, compound example 16.
1,3,5-Trihydroxy-4-prenylxanthone is a Na+/H+ exchange system (Na+/H+ Exchanger (NHE)) inhibitor with a minimum inhibitory concentration of 10 μg/mL[1]. 1,3,5-Trihydroxy-4-prenylxanthone is a phosphodiesterase type 5 (PDE5) (Phosphodiesterase (PDE)) inhibitor with an IC50 value of 3.0 μM[3]. 1,3,5-Trihydroxy-4-prenylxanthone inhibits Lipopolysaccharide (LPS) (Lipopolysaccharides (HY-D1056))-induced NO production in RAW264.7 macrophages, and has anti-inflammatory activities[2].
Zaragozic acid B, a fungal metabolite, is a potent inhibitor of both farnesyl-protein transferase (FPTase) and squalene synthases. Zaragozic acid B is a potential anticancer drug[1].
Palmitic acid-13C16 sodium is the 13C-labeled Palmitic acid sodium. Palmitic acid sodium is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid sodium can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
ER21355 is an inhibitor of phosphodiesterase 5 (PDE5), used for treatment of prostatic diseases.
Deoxyshikonin is isolated from Lithospermum erythrorhizon Sieb with antitumor activity. Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF, indicates a prolymphangiogenesis as well as a proangiogenesis effect in vitro[1]. Deoxyshikonin shows significant synergic antimicrobial activity with tetracycline against S. pneumonia (MIC=17 μg/mL), also shows significantly inhibitory activities against MRSA[2].
β-Apo-8'-carotenal (Apocarotenal), a provitamin A carotenoid, is an inducer of CYPlA1 and CYPlA2 in rat. β-Apo-8'-carotenal is present in many fruits and vegetables[1].
Irsenontrine (E2027) maleate is an orally active and selective phosphodiesterase 9 (PDE9) inhibitor. Irsenontrine maleate can be used for the research of neurological diseases[1][2].
Thienopyridone is a potent and selective phosphatase of regenerating liver (PRL) phosphatase inhibitor with IC50s of 173 nM, 277 nM and 128 nM for PRL-1, PRL-2, and PRL-3, respectively. Thienopyridone shows minimal effects on other phosphatases. Thienopyridone induces p130Cas cleavage and apoptosis and has anticancer effects[1].
hCAXII-IN-3 (Compound 6o) is a selective human carbonic anhydrase XII (hCAXII) inhibitor with a Ki of 10.0 nM[1].
(3S,5R)-Fluvastatin D6 sodium is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1]
Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders[1].
BergaptolA hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM. Recent studies suggest that it may have antiproliferative and anticancer properties.target: CYP3A4 [1]IC50: 24.92 [1]For in vivo enzyme activity analysis, 100 μM bergaptol was added to the cultures for an additional 24 h at 37°C. After centrifugation, the supernatant was used to measure the bergapten yield by high performance liquid chromatography (HPLC).[2]
α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a Kd value of 5.4 μM[1][2].
Cyanidin 3-arabinoside is a selective and reversible protein tyrosine phosphatase 1B (PTP1B) inhibitor, with an IC50 of 8.91 μM. Cyanidin 3-arabinoside is potential for the research of type 2 diabetes[1].
Hepatitis Virus C NS3 Protease Inhibitor 2 is a product-based peptide inhibitor of hepatitis C virus (HCV) NS3 protease, with a Ki of 41 nM[1].
MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.
XMD16-5 is a potent TNK2 inhibitor with IC50 values of 16 and 77 nM for the D163E and R806Q mutations, respectively.
hCAI/II-IN-4 (compound 6d) is a potent dual hCA I/II inhibitor with Ki values of 16.95, 15.22 and 27.04 nM for hCA I, hCA II and hCA Ⅸ, respectively. hCAI/II-IN-4 has anti-hypoxia activities and low toxicity. hCAI/II-IN-4 can be used for acute mountain sickness (AMS) research[1].
Lp-PLA2-IN-11 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-11 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2014114249A1, compound E145)[1].
Reproterol is a dual acting β2-adrenoceptor agonist and PDE inhibitor. The theophylline constituent of Reproterol inhibits phosphodiesterase activity induced by adenylyl cyclase. Reproterol has the potential for asthma research[1][2].
Fotagliptin is a Dipeptidyl Peptidase IV (DPP-4) inhibitor (IC50=2.27 nM). Fotagliptin displays great security in rat and dog. Fotagliptin can be used for Type 2 diabetes mellitus research[1].
Fexarine is a potent, non-steroidal and selective agonist of farnesoid X receptor (EC50: 38 nM). Fexarine can be used for the research of diseases linked to cholesterol, bile acids[1].
2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase.
NSC-87877 is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively[1]. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26)[2].
Garadacimab (CSL312) is a first-in-class, fully human IgG4 monoclonal antibody targeting activated factor XII (FXIIa). Garadacimab has the potential for hereditary angioedema research[1].
BMS-790052 is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture.IC50 Value: 9-50 pMTarget: HCV NS5ABMS-790052 has broad genotype coverage and exhibits picomolar in vitro potency against genotypes 1a (EC50 50pm) and 1b (EC50 9pm). BMS-790052 produces a robust decline in HCV RNA (-3.6 logs after 48 hours from a single 100 mg) dosefollowing a single dose in patients chronically infected with HCV genotype 1.