生物活性

• 描述The protein kinase C (PKC) family consists of at least 12 serine-threonine kinases and can be classified into three major groups: classical, novel, and atypical. Under physiological conditions, activation PKC is a response to various growth factors^[3]. Ro 31-8220 Mesylate is a potent inhibitor with IC50 values of 5nM, 24nM, 14nM, 27nM and 24nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively^[4]. In vitro, treatment with 3 μM Ro 31-8220 Mesylate significantly increased Akt/PKB phosphorylation at Ser 473 within 60 mins in A549 cells^[5]. Ro 31-8220 Mesylate activated JNK1 with EC50 value of 2.3 nM. Ro 31-8220 Mesylate also inhibited growth factor-stimulated c-Fos expression and amplified c-Jun expression in Rat-1 fibroblasts^[6]. Ro 31-8220 Mesylate diminished the 17AAG-induced clearance ErbB2 from the cell surface at the concentration of 1 μM in SKBR-3 cells^[7]. Treatment of hippocampal slice prior to DHPG administration with Ro 31-8220 Mesylate at the concentration of 1 μM significantly reduced the baseline PPF ratio by approximately 7%, indicating that inhibiting basal PKC activity increased presynaptic release in WT mice^[8].
• 作用机制Ro 31-8220 Mesylate carries a straight-chain alkyl side-chain bearing the cationic substituent which inhibits the PKC-α, PKC-β, PKC-γ and PKC-ε^[9].