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Staurosporine

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。

CAS号

62996-74-1

分子式

C28H26N4O3

主要靶点

Src|Antibacterial|PKC|Antibiotic|Apoptosis|Antifungal|PKA

仅限科研使用

Cat No : CM00517

Print datasheet

Synonyms

Staurosporine|STS|PKC|PKCη|PKCγ|PKCα|星孢菌素|星形孢菌素|Protein kinase A|Protein kinase C|PKA|c-Fgr|CGP 41251|CGP41251|CGP-41251|Bacterial|Antibiotic|Antibiotic AM 2282|Antibiotic AM2282|Antibiotic AM-2282|Apoptosis|AM2282|AM-2282|AM 2282|Fungal|inhibit|Inhibitor

验证数据展示

  • CAS No.: 62996-74-1

    Staurosporine
    CAS#: 62996-74-1

产品信息

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

CAS号 62996-74-1
分子式 C28H26N4O3
主要靶点 Src|Antibacterial|PKC|Antibiotic|Apoptosis|Antifungal|PKA
主要通路 凋亡|蛋白酪氨酸激酶|微生物学|微生物学|血管生成|蛋白酪氨酸激酶|细胞骨架|表观遗传|微生物学
分子量 466.53
纯度 99.24%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
别名 Staurosporine|STS|PKC|PKCη|PKCγ|PKCα|星孢菌素|星形孢菌素|Protein kinase A|Protein kinase C|PKA|c-Fgr|CGP 41251|CGP41251|CGP-41251|Bacterial|Antibiotic|Antibiotic AM 2282|Antibiotic AM2282|Antibiotic AM-2282|Apoptosis|AM2282|AM-2282|AM 2282|Fungal|inhibit|Inhibitor

靶点活性

CK2:19500 nM|EGFR:100 nM|PhK (Phosphorylase kinase):3 nM|PhK:3 nM|S6K:5 nM|PKA:15 nM|CK1:163500 nM|CSK:2000 nM|MLCK:21 nM|PKCε:73 nM|PKCζ:1086 nM|PKCγ:5 nM|ERK1:1500 nM|PKCα:2 nM|PKCδ:20 nM|PKCη:4 nM|TPK-IIB/Syk:16 nM|IR:61 nM|Ca 2+ /CaM PK-I1:20 nM|cdc2:9 nM|v-Src:6 nM|IGF-1R:6150 nM

体内活性

方法：为检测体内抗肿瘤活性，将 Staurosporine (3 mg/kg) 和 Lapatinib (50 mg/kg) 灌胃给药给携带人乳腺癌肿瘤 JIMT-1 的 Nu/J-Foxn1 Nu/Nu 小鼠，每周两次，持续两周。 结果：Staurosporine 和 Lapatinib 的组合以统计学显著的方式抑制了肿瘤生长。[4] 方法：为检测对胰岛 β 细胞功能的影响，将 Staurosporine (0.4 mg/kg in 0.5% sodium carboxymethyl cellulose) 腹腔注射给 iPLA2β-/-的 C57BL6 小鼠，每天一次，持续两周。 结果：Staurosporine 会损害动物的糖耐量和胰岛的葡萄糖刺激的胰岛素分泌。[5]

体外活性

方法：人宫颈癌细胞 HeLa 用 Staurosporine (1-10 nM) 处理 72 h，使用 MTT 方法检测细胞活力。 结果：Staurosporine 对 Hela 细胞增殖具有剂量依赖性抑制作用，IC50 约为 10 nM。[1] 方法：人胰腺癌细胞 PaTu 8988t、Panc-1 用 Staurosporine (1 μM) 处理 3-24 h，使用 Flow Cytometry 方法检测细胞死亡情况。 结果：PaTu 8988t 细胞，Staurosporine 孵育 3-24 h 显著增加了细胞凋亡率，并显著减少了生命细胞的数量；培养 6-16 h 后，坏死率增加。Panc-1 细胞，Staurosporine 处理在 9-24 h 后显著增加细胞凋亡并显著减少生命细胞的数量。[2] 方法：人肝癌细胞 HepG2 用 Staurosporine (20  nmol/L) 处理 6-24 h，使用 Western Blot 方法检测靶点蛋白表达水平。 结果：Staurosporine 显著抑制 mTOR 磷酸化并增加自噬标记蛋白 LC3-II 的表达，表明 Staurosporine 通过抑制 mTOR 有效激活自噬。[3]

溶解度

10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.1 mg/mL (6.64 mM);DMSO:31.56 mg/mL (67.65 mM);H2O:< 0.1 mg/mL (insoluble)

细胞实验

Cells are exposed to Staurosporine for ~32 hours. Cells are fixed in 4% paraformaldehyde and stained with the DNA-binding dye Hoechst 33342. Cells are visualized under epifluorescence illumination, and the percentage of apoptotic cells (cells with condensed and fragmented DNA) is determined. (Only for Reference)

参考文献

1.Ma X, et al. Staurosporine targets the Hippo pathway to inhibit cell growth. J Mol Cell Biol. 2018 Jun 1;10(3):267-269.
2.Malsy M, et al. Staurosporine induces apoptosis in pancreatic carcinoma cells PaTu 8988t and Panc-1 via the intrinsic signaling pathway. Eur J Med Res. 2019 Jan 28;24(1):5.
3.Ding Y, et al. Staurosporine suppresses survival of HepG2 cancer cells through Omi/HtrA2-mediated inhibition of PI3K/Akt signaling pathway. Tumour Biol. 2017 Mar;39(3):1010428317694317.
4.Zambrano JN, et al. Staurosporine, an inhibitor of hormonally up-regulated neu-associated kinase. Oncotarget. 2018 Nov 13;9(89):35962-35973.
5.Zhao Z, et al. Protection of pancreatic beta-cells by group VIA phospholipase A(2)-mediated repair of mitochondrial membrane peroxidation. Endocrinology. 2010 Jul;151(7):3038-48.
6.Yang J B, Song Y F, Liu Y, et al. UHPLC-QQQ-MS/MS assay for quantification of dianthrones as potential toxic markers of Polygonum multiflorum Thunb: Application to the standardization of TCMs with endogenous toxicity[J]. 2021
7.Xiao Q, Ye T, Wang X, et al. A network pharmacology-based study on key pharmacological pathways and targets of Qi Fu Yin acting on Alzheimer's disease[J]. Experimental Gerontology. 2021: 111336.

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