Inhibitors

Isorhamnetin-3-O-beta-D-Glucoside
Catalog No: CFN99757

Isorhamnetine-3-O-rutinoside inhibits the activity of alpha-glucosidase from rat intestine; it exhibits a potent rat lens aldose reductase (RLAR) inhibition in vitro, its IC(50) being 1.4 microM and has inhibitory effects of sorbitol accumulation, suggests that it is a leading compound for further study as a new drug for the prevention and/or treatment of diabetes and its complications.

Catharanthine
Catalog No: CFN99765

Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM, it dilates small mesenteric arteries and decreases heart rate and cardiac contractility by inhibition of voltage-operated calcium channels on vascular smooth muscle cells and cardiomyocytes.

Lupenone
Catalog No: CFN99681

Lupenone and lupeol inhibit protein tyrosine phosphatase 1B (PTP1B) with IC50 values of 13.7 ± 2.1 and 5.6 ± 0.9 uM, respectively, they are non−competitive inhibitors of PTP1B, and PTP1B appears to be an attractive target for the development of new drugs for type 2 diabetes and obesity. Lupenone stimulates melanogenesis by increasing the tyrosinase enzyme expression via mitogen-activated protein kinase phosphorylated extracellular signal-regulated kinases 1 and 2 phosphorylation inhibition. A 1 : 4 mixture of Lupenone and caryophyllene oxide shows trypanocidal activity.

Calyxin B
Catalog No: CFN99693

Calyxin B exhibits potent activity against human HT-1080 fibrosarcoma cells with an ED50 value of 0.69 microM. A methylated product of calyxin A and an epimeric mixture of Calyxin B, showed greatly reduced activity suggesting that phenolic hydroxyl groups are involved in the inhibitory activity.

Brevilin A
Catalog No: CFN99694

Brevilin A is a strong impetus for the development of selective JAK-STAT inhibitors and therapeutic drugs in order to improve survival of patients with hyperactivated JAKs and STATs. Brevilin A shows antigiardial activity (IC50 = 16.1 μM) and is similarly active in vitro against Entamoeba histolytica (IC50 between 4.5 and 9 μM) and against Plasmodium falciparum (IC50 = 9.42 μM).