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Staurosporine

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Chemical Structure| 62996-74-1 同义名 : 星孢菌素 ;STS;AM-2282;Staurosporin.;CGP-39360;CGP 41251;Antibiotic 230;Stsp;AM-2282，Antibiotic AM-2282;Antibiotic AM-2282
CAS号 : 62996-74-1
货号 : A256460
分子式 : C28H26N4O3
纯度 : 99%+
分子量 : 466.531
MDL号 : MFCD18252446
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(128.61 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 1.8 mg/mL clear

PO 0.5% CMC-Na 35 mg/mL suspension

生物活性
靶点

  • PKCη

    PKCη, IC50:4 nM

  • PKCγ

    PKCγ, IC50:5 nM

  • PKCε

    PKCε, IC50:73 nM

  • PKCα

    PKCα, IC50:2 nM

  • PKCδ

    PKCδ, IC50:20 nM
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].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
FL5.12-Akt1 cells Proliferation assay Antiproliferative activity against FL5.12-Akt1 cells by MTT assay, IC50=0.29 μM. 16403626
HEK293 cells Cytotoxic assay 72 h Cytotoxicity against HEK293 cells after 72 hrs by CellTiterGlo assay, IC50=56 nM. 24763262
HEK293 cells Function assay Inhibition of IL-8 release by HEK293 cells expressing PKC-beta2, IC50=77 nM. 15771419
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00651261 Leukemia Phase 3 Active, not recruiting - -
NCT01161550 Leukemia, Myeloid, Acute Phase 1 Completed - United States, Missouri ... 展开 >> Washington University School of Medicine St. Louis, Missouri, United States, 63110 收起 <<
NCT00019838 Leukemia Lymp... 展开 >>homa 收起 << Phase 1 Completed - United States, Maryland ... 展开 >> Warren Grant Magnuson Clinical Center - NCI Clinical Studies Support Bethesda, Maryland, United States, 20892-1182 NCI - Center for Cancer Research Bethesda, Maryland, United States, 20892 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.72mL

2.14mL

1.07mL

21.43mL

4.29mL

2.14mL
参考文献

[1]Tamaoki T, Nomoto H, et al. Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase. Biochem Biophys Res Commun. 1986 Mar 13;135(2):397-402.

[2]Meggio F, Donella Deana A, et al. Different susceptibility of protein kinases to staurosporine inhibition. Kinetic studies and molecular bases for the resistance of protein kinase CK2. Eur J Biochem. 1995 Nov 15;234(1):317-22.

[3]Wolf M, Baggiolini M, et al. The protein kinase inhibitor staurosporine, like phorbol esters, induces the association of protein kinase C with membranes. Biochem Biophys Res Commun. 1988 Aug 15;154(3):1273-9.

[4]Ōmura S, Asami Y, et al. Staurosporine: new lease of life for parent compound of today's novel and highly successful anti-cancer drugs. J Antibiot (Tokyo). 2018 Aug;71(8):688-701.

[5]Secrest RJ, Williams P, et al. Hypotensive properties of the protein kinase inhibitor, staurosporine, in normotensive and spontaneously hypertensive rats. Clin Exp Hypertens A. 1991;13(2):219-34.

[6]Gurley LR, Umbarger KO, et al. High-performance liquid chromatographic analysis of staurosporine in vivo. Its translocation and pharmacokinetics in rats. J Chromatogr B Biomed Sci Appl. 1998 Aug 7;712(1-2):211-24.