产品描述:
Gambogic acid (GA) is a xanthonoid that has been found in G. hanburyi resin and has anticancer activity.{49693,23527,23530} It binds covalently to the regulatory subunit B (SPTSSB) of the serine palmitoyltransferase complex (Ki = 1.5 µM; kinact = 0.05 min-1) and inhibits de novo sphingolipid biosynthesis.{49693} GA activates caspases in T47D breast cancer cells (EC50 = 0.78 µM) and inhibits binding of anti-apoptotic proteins to a BH3 peptide (IC50s = 1.47, 1.21, 2.02, 0.66, 1.06, and 0.79 μM for Bcl-xL, Bcl-2, Bcl-W, Bcl-B, Bfl-1, and Mcl-1, respectively), as well as decreases the expression of Bcl-2 and increases the expression of Bax in MGC-803 human gastric carcinoma cells.{23529,23528,23526} GA binds to the transferrin receptor (IC50 = 4.1 µM), reduces growth of a variety of cancer cell lines (GI50s = 0.115-1 µM), and induces apoptosis in T47D cells.{23527} It also inhibits growth of U87 glioma cells, as well as increases the levels of leucine-rich repeats and immunoglobulin-like domains protein 1 (LRIG1), decreases the levels of EGFR, and reduces Akt/mTORC1 signaling in these cells.{23530} GA inhibits the chymotrypsin activity of the 20S proteasome in a dose-dependent manner and is a slow inhibitor of inward-rectifying potassium channel 2.1 (Kir2.1; IC50 = <0.1 µM).{23531,23524}