D-Tyrosine-d7 is the deuterium labeled D-Tyrosine. D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth[1][2].
Oxyresveratrol 2-O-β-D-glucopyranoside is a phenolic compound isolated from Morus nigra root and is an effective tyrosinase inhibitor with an IC50 of 29.75 μM[1].
Thrombin receptor peptide ligand is a thrombin receptor antagonist peptide that can be used as an antithrombotic agent[1].
Doxycycline calcium, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor[1]. Doxycycline calcium shows antibacterial activity and anti-cancer cell proliferation activity[1][2][3][4][5].
LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines[1].
Quinidine polygalacturonate is an antiarrhythmic agent. Quinidine polygalacturonate is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine polygalacturonate is also a K+ channel blocker with an IC50 of 19.9 μM, and can induce apoptosis. Quinidine polygalacturonate can be used for malaria research[1][2][3][4].
Enocyanin is an anthocyanin extracted from grapes. Enocyanin shows inhibitory effect on the leucine aminopeptidase, acid phosphatase, γ-glutamyl transpeptidase and esterase activity[1].
(3S,5S)-Atorvastatin sodium salt is a pregnane X receptor (PXR) activator and the inactive enantiomer of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor with lipid-lowering capabilities[1].
4-Ethynyl-L-phenylalanine is a selective, reversible, potent and competitive inhibitor of tryptophan hydroxylase (TPH). 4-Ethynyl-L-phenylalanine is a competitive inhibitor with regard to the substrate tryptophan, with a Ki of 32.6 μM. 4-Ethynyl-L-phenylalanine selectively and reversibly inhibits the biosynthesis of serotonin[1].
YCT529 free acid is a potent, selective and orally active RAR-α inhibitor[1].
IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2[1].
Anticancer agent 65 (compound 4c) shows excellent activity in cancer cell lines, especially A549 cells, with an IC50 of 1.07 μM. Anticancer agent 65 induces S-phase arrest in A549 cells and increases the expression level of p53 and p21. Anticancer agent 65 causes apoptosis, ROS generation and collapse of MMP in A549 cells[1].
1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects[1][2].
Terlakiren (CP-80,794) is an orally active inhibitor of renin. Terlakiren inhibits the efficacy of human renin with an IC50 value of 0.7 nM. Terlakiren has potential applications in hypertension[1].
AT-533 is a potent Hsp90 and HSV inhibitor. AT-533 suppresses tumor growth and angiogenesis by blocking the HIF-1α/VEGF/VEGFR-2 signaling pathway. AT-533 also inhibits the activation of the downstream pathways, including Akt/mTOR/p70S6K, Erk1/2 and FAK. AT-533 inhibits the tube formation, cell migration, and invasion of human umbilical vein endothelial cells (HUVECs)[1][2][3].
Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril (AHU-377) is a component of the heart failure medicine LCZ696.
FXR agonist 5 (compound 1) is a FXR agonist. FXR agonist 5 can be used for research in diseases or disorders caused by metabolic inflammation[1].
ML-211 is a carbamate-based dual inhibitor of acyl-protein thioesterase 1 (APT1)/lysophospholipase 1 (LYPLA1) (IC50=17 nM) and LYPLA2 (IC50=30 nM). ML-211 also inhibits theserine hydrolase ABHD11 with an IC50 value of 10 nM but is ≥ 50-fold selective for LYPLA in a panel of 20 additional serine hydrolases[1].
JG26 is an ADAM17 inhibitor, with IC50 values of 12 nM, 1.9 nM, 150 nM and 9.4 nM for ADAM8, ADAM17, ADAM10 and MMP-12, respectively[1].
Evogliptin tartrate is a potent, orally bioavailable and selective dipeptidyl peptidase-4 (DPP-4) inhibitor, with antidiabetic activity. Evogliptin tartrate has potential for anti-atherosclerosis therapy that targets arterial inflammation[1].
P32/98 is a potent inhibitor of dipeptidyl peptidase IV. P32/98 improves glucose tolerance, insulin sensitivity and β-cell responsiveness in preclinical studies using the fatty Zucker rat, an animal model for IGT (impaired glucose tolerance)[1].
PCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC50 value of 6.4 µM. PCSK9-IN-10 increases the expression of LDLR protein and decreases the expression of PCSK9. PCSK9-IN-10 reduces atherosclerosis progression. PCSK9-IN-10 has the potential for the research of hyperlipidemia[1].
Marimastat is a broad spectrum inhibitor of MMPs with IC50 values of 3, 5, 6, 9 and 13 nM for MMP-9, MMP-1, MMP-2, MMP-14 and MMP-7, respectively.
CP-640186 is an isozyme-nonselective acetyl-CoA carboxylase (ACCase) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively; with improved metabolic stability vs CP-610431.IC50 value: 53 nM/61 nM (rat liver ACC1/skeletal muscle ACC2) [1]Target: acetyl-CoA carboxylasein vitro: CP-640186, also inhibited both isozymes with IC50s of ~55 nM but was 2–3 times more potent than CP-610431 in inhibiting HepG2 cell fatty acid and TG synthesis. CP-640186 also stimulated fatty acid oxidation in C2C12 cells (ACC2) and in rat epitrochlearis muscle strips with EC50s of 57 nM and 1.3 uM [1]. in vivo: In rats, CP-640186 lowered hepatic, soleus muscle,quadriceps muscle, and cardiac muscle malonyl-CoAwith ED50s of 55, 6, 15, and 8 mg/kg. Consequently, CP-640186 inhibited fatty acid synthesis in rats, CD1 mice,and ob/ob mice with ED50s of 13, 11, and 4 mg/kg, andstimulated rat whole body fatty acid oxidation with anED50 of ~30 mg/kg [1].
cis-ACCP is an orally active antimetastatic matrix metalloproteinase-2 (MMP-2) selective inhibitor. cis-ACCP can inhibit MMP-2 and MMP-9 with IC50 values of 4 μM and 20 μM, respectively. cis-ACCP can be used for the research of a variety of chronic diseases[1].
Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis[1][2][4].
Moracin P is a 2-arylbenzofuran isolated from the Mori Cortex Radicis. Moracin P exhibits potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1). Moracin P reduces oxygen-glucose deprivation (OGD)-induced reactive oxygen species (ROS) production. Moracin P has neuroprotective and anti-inflammatory effects[1][2][3].
(S)-Indoximod-d3 is the deuterium labeled (S)-Indoximod. (S)-Indoximod (1-Methyl-L-tryptophan) is an inhibitor of indoleamine 2,3-dioxygenase (IDO). (S)-Indoximod can be used for the research of cancer[1][2][3].
Vildagliptin carboxylic acid metabolite (M20.7) TFA is a potent P450 enzyme activity inhibitor[1].
CH3OCO-D-CHA-Gly-Arg-pNA acetate is a chromogenic substrate for factor Xa[1][2].