Fascaplysin is an inhibitor of cyclin D kinase 4/ cyclin D1 (IC50 = 0.35 μM) that was originally isolated from the marine sponge Thorectandra.
CAS:114719-57-2
分子式:C18H11N2O.Cl
分子量:306.8
纯度:98%
存储:Store at -20°C
Background:
Fascaplysin is an inhibitor of cyclin D kinase 4/ cyclin D1 (IC50 = 0.35 μM) that was originally isolated from the marine sponge Thorectandra. It is significantly less selective for Cdk6/cyclin D1 (IC50 = 3.4 μM) and does not inhibit other Cdks and tyrosine kinases. Fascaplysin is reported to have antiproliferative activity against retinoblastoma-positive tumor cells, blocking retinoblastoma phosphorylation and inducing G1 arrest. Inhibition of Cdk4 via fascaplysin has been shown to induce peroxisome-proliferator-activated receptor γ-1α deacetylation (IC50 = 0.7 uM) and has been used to demonstrate a role for insulin-activated cyclinD1-Cdk4 signaling in the control of glucose metabolism.