PTP1B Inhibitor

Licoflavone A is an orally active PTP1B/VEGFR-2 inhibitor, with an IC₅₀ of 54.5 μM against PTP1B, an IC₅₀ of 14.36 μM and a K_d of 142.38 nM against human VEGFR-2. Licoflavone A blocks the PI3K/AKT and MEK/ERK signaling pathways. Licoflavone A induces G1 phase cell cycle arrest, apoptosis via the intrinsic mitochondrial pathway (apoptosis), and inhibits migration, invasion and epithelial-mesenchymal transition (EMT) of gastric cancer cells. Licoflavone A inhibits the proliferation of gastric cancer cells in vitro and in xenograft models. Licoflavone A reduces the expression levels of HIF-1α, GLUT1, LDHA, PKM2 and HK2 in hypoxic gastric cancer cells, decreases glucose uptake and suppresses glycolysis. Licoflavone A can be used in research related to gastric cancer, type 2 diabetes and obesity.

(Z)-2-(Oleoyloxy) propane-1,3-diyl dipalmitate (1,3-Dipalmitoyl-2-oleoylglycerol) is an orally active PTP1B inhibitor with an IC₅₀ of 31.01 μM and a K_i of 16.36 μM. (Z)-2-(Oleoyloxy) propane-1,3-diyl dipalmitate also inhibits α-glucosidase with an IC₅₀ of 163.31 μM. It inhibits phosphorylation of p38 MAPK, activates the PI3K/Akt/CREB pathway, and exhibits antioxidant, anti-apoptosis and anti-inflammatory activities, as well as inhibits peroxynitrite-mediated albumin nitration. (Z)-2-(Oleoyloxy) propane-1,3-diyl dipalmitate can be used in studies related to cerebral ischemia-reperfusion injury and diabetes.

PTP1B-IN-35 is an orally active protein tyrosine phosphatase 1B (PTP1B) inhibitor, with an IC₅₀ of 32.7 μM, a K_is of 18.8 μM, a K_ii of 45.3 μM, and a K_d of 36 μM against human PTP1B. PTP1B-IN-35 promotes glucose uptake, improves glucose tolerance, enhances insulin sensitivity, and reduces blood glucose levels. PTP1B-IN-35 can be used in the research of type 2 diabetes.

PTP1B/TC-PTP IN-1 is a PTP1B and TC-PTP dual inhibitor. PTP1B/TC-PTP IN-1 can be used as a target protein ligand for the synthesis of DU-14 (PTP1B/TC-PTP PROTAC) (HY-164864).

4',7-Dihydroxy-3'-methoxyflavanone is a protein tyrosine phosphatase 1B (PTP1B) inhibitor, with an IC₅₀ of 98.1 μM against human targets. 4',7-Dihydroxy-3'-methoxyflavanone can be used in research related to type 2 diabetes and obesity.