Cayman DAPH

DAPH is a phthalimide with diverse biological activities.^,,, 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. It also inhibits EGFR autophosphorylation in A431 human epidermoid carcinoma cell membranes and intact cells (IC₅₀s = 1 and <10 μM, respectively). DAPH inhibits contractions induced by phenylephrine (Item No. ) in isolated rat endothelium-denuded aortic rings in a concentration-dependent manner. It inhibits aggregation of amyloid-β (1-42) (Aβ42) peptide (Item No. ), disaggregates preformed Aβ42 fibrils, and inhibits calcium influx into mouse CATH.a neuronal cells when used at a concentration of 10 μM. 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).

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information regarding the kinase IC₅₀ values and reduction in EGFR autophosphorylation was drawn from a paper that has been retracted; however, the information specified in the retraction statement has not been included.

WARNING This product is not for human or veterinary use.