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背景说明：Malantide TFA 是一种合成的十二肽，由被磷酸化酶激酶β亚基上的 PKA 磷酸化的位点衍生而来。Malantide TFA 是 PKA 的高度特异性底物，Km 为 15 μM，并且在各种大鼠组织提取物中显示出 PKI 抑制 > 90％底物磷酸化。Malantide TFA 也是 PKC 的有效底物，Km 为 16 μM。 Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide TFA is also an efficient substrate for PKC with a Km of 16 μM[2].
In Vitro：The Km values of Malantide are 15 μM and 223 μM for PKA and PKG, respectively. The Vmax values are 23.8 units/mg and 6.6 units/mg for for PKA and PKG, respectively.
A statistically significant effect of isoprenaline on the activity ratio of guinea-pig heart was only: observed with Malantide.
参考文献：[1] K J Murray, et al. Use of a Synthetic Dodecapeptide (Malantide) to Measure the Cyclic AMP-dependent Protein Kinase Activity Ratio in a Variety of Tissues. Biochem J. 1990 May 1;267(3):703-8.
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