phosphorylase kinase

K-252a is a staurosporine analog isolated from Nocardiopsis sp. soil fungi. K-252a inhibits protein kinase (IC50: 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+ calmodulin-dependent kinase type II, and phosphorylase kinase, respectively).

Phosphorylase Kinase β-Subunit Fragment (420-436) is a peptide fragment (430-436) derived from the β-Subunit of phosphorylase kinase. Phosphorylase kinase, a serine threonine-specific protein kinase, plays a crucial role in the activation of glycogen phosphorylase for the release of glucose-1-phosphate from glycogen[1].

Staurosporine (AM-2282) 是一种蛋白激酶抑制剂，对 PKC、PKA、c-Fgr、Phosphorylase kinase 和 TAOK2 均有抑制活性 (IC50=6 15 2 3 3000 nM)，具有 ATP 竞争性和非选择性。Staurosporine 也可以诱导凋亡。

Disodium monofluorophosphate (NSC248) 是丙酮酸激酶和碱性磷酸酶的竞争性抑制剂，它也不可逆地抑制磷酸化酶磷酸酶。

N6-Methyladenosine 5'-monophosphate disodium salt 是糖原磷酸化酶 b 激活剂，也是腺苷酸激酶 II 的抑制剂。

7-oxo Staurosporine is an antibiotic originally isolated from S. platensis with diverse biological activites. It inhibits PKC, PKA, phosphorylase kinase, EGFR, and c-Src in vitro (IC50s = 9, 26, 5, 200, and 800 nM, respectively). 7-oxo Staurosporine induces cell cycle arrest in the G2/M phase in human leukemia K562 cells with a minimal effective dose (MED) of 30 ng/ml. It is cytotoxic to P388 mouse leukemia cells that are resistant and susceptible to doxorubicin . 7-oxo Staurosporine inhibits growth of the mycelial, but not yeast form of C. albicans, C. krusei, C. tropicalis, and C. lusitaniae (MICs = 3.1-25 μg/ml). It increases sphingomyelin synthesis in CHO-K1 cells when used at a concentration of 50 nM.

The cyanobacterium Nodularia spumigena often contaminates the drinking water of rural communities in developing countries and accumulates in mussels, flounder, and cod from the northern Baltic Sea. Nodularin is a hepatotoxic monocylic pentapeptide produced by the N. spumigena. It is a potent inhibitor of protein phosphatase types 1 (PP1) and 2A (PP2A), exhibiting IC50 values of 1.8 and 0.026 nM, respectively. PP2B is inhibited to a lesser extent with an IC50 of 1.8 μM. No apparent inhibitory effect is observed with PP2C, alkaline phosphatase, acid phosphatase, insulin receptor tyrosine kinase, protein kinase A, phosphorylase kinase, or protein kinase C.

5-Iodotubercidin (NSC-113939) 是一种 ATP 类似物，有效抑制腺苷激酶，IC50为 26 nM。它可以激活磷酸化酶和糖原合成酶，在离体肝细胞中启动糖原合成。它也抑制 CK1、胰岛素受体酪氨酸激酶、磷酸化酶激酶、PKA、CK2、PKC 和 Haspin 。

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。

Myelin Basic Protein (MHP4-14) TFA 是一种合成肽，包含髓鞘碱性蛋白的残基4-14，是一种非常有选择性的 PKC 底物 (Km=7 μM)。Myelin Basic Protein TFA 不被环腺苷酸依赖性蛋白激酶、酪蛋白激酶 I 和 II、Ca2+ 钙调素依赖性蛋白激酶 II 或磷酸化酶激酶磷酸化，可常规用于测定粗组织提取物中低背景的蛋白激酶 C。

Rp-Adenosine-5'-O-(1-thiodiphosphate)（Rp-ADP-α-S）是ADP-α-S的含硫异构体，是磷酸化酶激酶的抑制剂（Ki = 0.53 µM）。此化合物能诱导分离的人类血小板聚集（EC50 = 20 µM），并能引发经卡巴胆碱预收缩的豚鼠乙状结肠松弛（EC50 = 58.9 µM）。

Sp-Adenosine-5’-O-(1-thiodiphosphate) (Sp-ADP-α-S) 是硫含量核苷酸衍生物ADP-α-S的一种异构体。它是磷酸化酶激酶的抑制剂（Ki = 0.53 µM）。Sp-ADP-α-S能引起人类孤立血小板聚集（EC50 = 20 µM），并能使羧胺胆碱预收缩的豚鼠taenia coli松弛（EC50 = 58.9 µM）。