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星形孢菌素 /Staurosporine {[allProObj[0].p_purity_real_show]}

货号:A256460 同义名: 星孢菌素 / STS;AM-2282

Staurosporine是一种典型的强效ATP竞争性多激酶抑制剂,IC50值为0.7 nM(PKC)、7 nM(PKA)、8.5 nM(PKG)、6 nM(p60v-src酪氨酸蛋白激酶)、20 nM(CaM激酶II)。

Staurosporine 化学结构 CAS号:62996-74-1
Staurosporine 化学结构
CAS号:62996-74-1
Staurosporine 3D分子结构
CAS号:62996-74-1
Staurosporine 化学结构 CAS号:62996-74-1
Staurosporine 3D分子结构 CAS号:62996-74-1
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Staurosporine 纯度/质量文件 产品仅供科研

货号:A256460 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 PKC PKCα PKCβ PKCγ PKCδ PKCε PKCζ PKCη PKCθ 其他靶点 纯度
Daphnetin +

PKC, IC50: 25.01 μM

EGFR,PKA 95%
Dequalinium Chloride 99%+
Quercetin Sirtuin,Src 97%
Myricetrin 96%
Go 6983 +++

PKCα, IC50: 7 nM

+++

PKCβ, IC50: 7 nM

+++

PKCγ, IC50: 6 nM

+++

PKCδ, IC50: 10 nM

++

PKCζ, IC50: 60 nM

99%+
Go6976 +++

PKC, IC50: 7.9 nM

++++

PKCα, IC50: 2.3 nM

+++

PKCβ1, IC50: 6.2 nM

FLT3 99%+
Bisindolylmaleimide I +++

PKCα, IC50: 20 nM

+++

PKCβ1, IC50: 17 nM

PKCβ2, IC50: 16 nM

+++

PKCγ, IC50: 20 nM

99%+
Lawsone methyl ether 99%
Sotrastaurin ++++

PKCα, Ki: 0.95 nM

++++

PKCβ1, Ki: 0.64 nM

++++

PKCδ, Ki: 2.1 nM

++++

PKCε, Ki: 3.2 nM

++++

PKCη, Ki: 1.8 nM

++++

PKCθ, Ki: 0.22 nM

99%+
Enzastaurin ++

PKCα, IC50: 39 nM

+++

PKCβ, IC50: 6 nM

+

PKCγ, IC50: 83 nM

+

PKCε, IC50: 110 nM

98%
Midostaurin ++

PKCα, IC50: 22 nM

++

PKCβ1, IC50: 30 nM

PKCβ2, IC50: 31 nM

++

PKCγ, IC50: 24 nM

+

PKCδ, IC50: 330 nM

+

PKCε, IC50: 1.25 μM

+

PKCη, IC50: 160 nM

99%
Ro 31-8220 mesylate ++++

PKCα, IC50: 5 nM

+++

PKCβ1, IC50: 24 nM

PKCβ2, IC50: 14 nM

++

PKCγ, IC50: 27 nM

++

PKCε, IC50: 24 nM

99%+
Staurosporine ++++

PKCα, IC50: 2 nM

++++

PKCγ, IC50: 5 nM

+++

PKCδ, IC50: 20 nM

++

PKCε, IC50: 73 nM

++++

PKCη, IC50: 4 nM

99%+
Ruboxistaurin HCl +

PKCα, IC50: 0.36 μM

++++

PKCβ1, IC50: 4.7 nM

PKCβ2, IC50: 5.9 nM

+

PKCγ, IC50: 0.3 μM

+

PKCδ, IC50: 0.25 μM

++

PKCη, IC50: 0.052 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 ALK1 ALK2 ALK3 ALK4 ALK6 Smad3 TGF-β TGFβRI/ALK5 TGFβRII 其他靶点 纯度
LDN193189 ++++

ALK1, IC50: 0.8 nM

++++

ALK2, IC50: 0.8 nM

+++

ALK3, IC50: 5.3 nM

+++

ALK6, IC50: 16.7 nM

99%+
LDN-212854 ++++

ALK1, IC50: 2.4 nM

++++

ALK2, IC50: 1.3 nM

+

ALK3, IC50: 85.8 nM

+

ALK4, IC50: 2133 nM

+

ALK5, IC50: 9276 nM

99%+
ML347 ++

ALK1, IC50: 46 nM

++

ALK2, IC50: 32 nM

98%
K02288 ++++

ALK1, IC50: 1.8 nM

++++

ALK2, IC50: 1.1 nM

++

ALK3, IC50: 34.4 nM

+++

ALK6, IC50: 6.4 nM

99%+
LDN-193189 dihydrochloride ++++

ALK1, IC50: 0.8 nM

++++

ALK2, IC50: 0.8 nM

+++

ALK3, IC50: 5.3 nM

+++

ALK6, IC50: 16.7 nM

99%
LDN-214117 ++

ALK2, IC50: 24 nM

98%
DMH-1 +

ALK2, IC50: 107.9 nM

99%+
SB-505124 +

ALK4, IC50: 129 nM

++

ALK5, IC50: 47 nM

99%+
Vactosertib +++

ALK4, IC50: 13 nM

+++

ALK5, IC50: 11 nM

99%+
Alantolactone 98%
SIS3 97%
Pirfenidone 98%
Hesperetin 97%
RepSox ++++

TGFβR1(ALK5), IC50: 4 nM

98%
GW788388 +++

ALK5, IC50: 18 nM

98%
LY364947 ++

TGFβRI, IC50: 59 nM

+

TGFβRII, IC50: 0.4 μM

98%
SD-208 ++

TGF-βRI (ALK5), IC50: 48 nM

99%
SB-525334 +++

TGFβR1(ALK5), IC50: 14.3 nM

99%+
LY2109761 ++

TβRI, Ki: 38 nM

+

TβRII, Ki: 300 nM

99%+
Galunisertib ++

TβRI, IC50: 56 nM

98%
SB 431542 +

ALK5, IC50: 94 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Staurosporine 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].

Staurosporine 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
HEK293 cells Cytotoxic assay Cytotoxicity against HEK293 cells, EC50=2 μM. 25316317

Staurosporine 动物研究

Dose Rat[5] (i.v.): min = 0.1 mg/kg, max = 10 mg/kg
Administration i.v.
Pharmacokinetics
Animal Rats[6]
T1/2 51.6 min (in plasma)
75.3 min (in RBC)

Staurosporine 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 <<

Staurosporine 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.

Staurosporine 实验方案

计算器
存储液制备 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

Staurosporine 技术信息

CAS号62996-74-1
分子式C28H26N4O3
分子量 466.531
别名 星孢菌素 ;STS;AM-2282;Staurosporin.;CGP-39360;CGP 41251;Antibiotic 230;Stsp;AM-2282,Antibiotic AM-2282;Antibiotic AM-2282
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

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

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

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