Gigantol

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Gigantol 是一种新型 Wnt/β-catenin 通路抑制剂。它通过下调乳腺癌细胞中磷酸化的 LRP6 和胞质 β-连环蛋白来抑制 Wnt/β-连环蛋白信号传导。

Gigantol is a novel inhibitor of the Wnt/β-catenin pathway. It inhibits Wnt/β-catenin signaling through downregulation of phosphorylated LRP6 and cytosolic β-catenin in breast cancer cells. Gigantol may be developed as a promising neuroprotective agent for successful MSC transplantation in ischemic diseases, it shows the protective effect against hydrogen peroxide-induced apoptosis in rat bone marrow mesenchymal stem cells through the PI3K/Akt pathway.Gigantol inhibits aldose reductase gene to exert its anti-cataract activity. Gigantol induces growth inhibition and apoptosis of HepG2 cells via the PI3K/Akt/NF-κB signaling pathway.Gigantol also shows α-glucosidase inhibitory activity.

Gigantol isomer-1 decreases the level of phosphorylated LRP6 and cytosolic β-catenin in HEK293 cells. In breast cancer MDA-MB-231 and MDA-MB-468 cells, treatment with Gigantol isomer-1 reduces the level of phosphorylated LRP6. Gigantol isomer-1 significantly inhibits the proliferation and induces apoptosis of the HepG2 cells. Gigantol isomer-1 at concentrations of 1, 40 and 150 μM markedly decreases the cell viability by 11.7, 30.0 and 56.4% at 24 h and 21.1, 66.8 and 85.5% at 48 h, respectively. The IC50 value is 9.30 μM.

LDD and Gigantol isomer-1 (25–100 mg/kg, p.o.) significantly increase the hot-plate latency in comparison to vehicle-treated mice and decreased carrageenaninduced inflammation in rats.

——

Others

Other Targets

β-catenin| α-glucosidase

Cancer

——

67884-30-4

274.31

C16H18O4

>98% (HPLC)

DMSO : ≥ 160 mg/mL; 583.28 mM

COc1cc(O)cc(CCc2ccc(OC)c(O)c2)c1

——

(-20℃)

With Ice Pack

≥ 2 years