产品描述:
DAPH is a phthalimide with diverse biological activities.{47738,47739,47740,47741} It is an EGFR inhibitor that selectively inhibits the EGFR intracellular kinase domain over v-Abl, c-Src, PKCα, PKCβ1, PKCβ2, and PKCγ (IC50s = 0.3, >50, 16, 6, 30, 4.8, and 30 μM, respectively) and a panel of 11 other kinases.{47738} It also inhibits EGFR autophosphorylation in A431 human epidermoid carcinoma cell membranes and intact cells (IC50s = 1 and 17205) in isolated rat endothelium-denuded aortic rings in a concentration-dependent manner.{47739} It inhibits aggregation of amyloid-β (1-42) (Aβ42) peptide (Item No. 20574), disaggregates preformed Aβ42 fibrils, and inhibits calcium influx into mouse CATH.a neuronal cells when used at a concentration of 10 μM.{47740} DAPH also inhibits aggregation of a Sup35 yeast prion protein fragment that contains its N-terminal and highly charged middle domains (IC50 = 0.58 μM).{47741} The information regarding the kinase IC50 values and reduction in EGFR autophosphorylation was drawn from a paper that has been retracted; however, the information specified in the retraction statement has not been included.{47738}