Inhibitors

Aucubin
Catalog No: CFN98530

Aucubin is an iridoid glycoside with a wide range of biological activities, including pancreas-protective, chondroprotective, antispasmodic, liver-protective, anti-inflammatory, anti-microbial, antioxidant, anti-algesic as well as anti-tumor activities. Aucubin prevents neuronal death in the hippocampal CA1 region in rats with diabetic encephalopathy, it also has protective effects on H2O2-induced apoptosis in PC12 cells. Aucubin may improve obesity-induced atherosclerosis by attenuating TNF-α-induced inflammatory responses. Aucubin suppresses hepatitis B viral DNA replication in vitro.

3-Acetoxy-11-ursen-28,13-olide
Catalog No: CFN98487

3β-Acetoxy-urs-11-en-28,13-olide exhibits significant protein tyrosine phosphatase 1B (PTP1B) inhibitory activity, it is a mixed-type PTP1B inhibitor. It exhibits weak-moderate antiproliferative activity against the A2780 human ovarian cancer cell line.

Miltirone
Catalog No: CFN98531

Miltirone is a CYPs inhibition, it has been characterized as a low-affinity ligand for central benzodiazepine receptors, it might ameliorate the symptoms associated with discontinuation of long-term administration of ethanol or of other positive modulators of the GABA A receptor. Miltirone possesses significant anticancer, antibacterial, antioxidant, and anti-inflammatory activities, the hepatocyte metabolism is the major route of clearance for miltirone. Miltirone is collateral sensitive in multidrug-resistant P-gp-overexpressing cells, induces G2/M arrest, and triggeres apoptosis via ROS-generated breakdown of MMP and DNA damage. Miltirone has antiprotozoal activity against T. brucei rhodesiense STIB 900.

Digoxin
Catalog No: CFN98536

Digoxin is a classical Na,K-ATPase inhibitor, with selectivity for the α2β3 isoform over the common α1β1 isoform, used in the treatment of atrial fibrillation and heart failure. Digoxin and other cardiac glycosides can inhibit hypoxia-inducible factor 1 (HIF-1)α synthesis and block tumor growth.

N-p-trans-Coumaroyltyramine
Catalog No: CFN98494

N-p-trans-Coumaroyltyramine is an inhibitor on acetylcholinesterase (AChE), it inhibits AChE activity in a dose-dependent manner with IC50 value of 34.5 microg/mL (122 microM). It exhibits potent inhibition of cell proliferation, platelet aggregation, and shows antioxidant activity. N-trans-p-coumaroyltyramine shows activity against Trypanosoma brucei rhodesiense (IC50s ranging from 2.2 to 13.3 microM).