生物活性

• 靶点

  CaMKII IC50:20nM

  PKA IC50:7nM

  PKC IC50:0.7nM

  PKG IC50:8.5nM

  v-Src (p60) IC50:6nM

• 描述Protein kinase C (PKC) is a serine/threonine protein kinase, which plays a crucial role in signaling transduction mechanisms in many cell types and tissues. Staurosporine is the first reported and widely used PKC inhibitor with IC50 value of 2.7 nM for PKC (rat brain, measured by enzyme activity assay)^[1] and also displays broadly potent across the kinome with IC50 values of 15 nM, 18 nM, 3 nM, 5 nM, 21 nM, 20 nM, 9 nM, 6 nM, 20 nM, 2 nM, 16 nM for PKA, PKG, Phosphorylase kinase, S6 kinase, MLCK, Ca²⁺/CaM PK-II, cdc2, v-Src, Lyn, c-Fgr, TPK-IIB/Syk (measured by recombinant enzyme), respectively. Staurosporine is a broad selective protein kinase inhibitor and can suppress the auto-phosphorylation of Lyn and c-Fgr in a dose-dependent manner^[2]. Staurosporine induces the translocation of PKC from the soluble to the membrane, considered as the inactivation of PKC, and causes the Inhibition of PKC activity with decreased phosphorylation of PKC substrate. The inhibition of staurosporine against PKC is Ca²⁺ dependent^[3]. Staurosporine can disturb different cell response, including neuronal function, cell growth and differentiation, cell motility, secretion and cellular metabolism and smooth muscle contraction, through inhibition of PKC^[4].
• 作用机制Staurosporine is an ATP-competitive inhibitor of PKC^[2].

• 动物研究
  剂量	Rat[5] (i.v.): min = 0.1 mg/kg, max = 10 mg/kg
  给药途径	i.v.
  动物药代数据	Animal Rats[6] T1/2 51.6 min (in plasma) 75.3 min (in RBC)