Staurosporine

Staurosporineは1種の有効なPKC阻害剤で、無細胞試験でPKCα、PKCγ とPKCηに作用します。そして、これらのIC50値は2 nM、5 nM と 4 nMそれぞれに分かれます。StaurosporineはPKCδ(20 nM)とPKCε(73 nM)に作用することが弱くて、PKCζ (1086 nM)に対する活性も低いですが、他のキナーゼ(例えば、PKA、PKG、S6K、CaMKII等)に抑制活性を現れます。臨床3期。

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Staurosporine 化学構造
分子量: 466.53

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製品説明

  • Compare PKC Inhibitors
    PKC製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法
  • Staurosporineのメカニズム

製品の説明

生物活性

製品説明 Staurosporineは1種の有効なPKC阻害剤で、無細胞試験でPKCα、PKCγ とPKCηに作用します。そして、これらのIC50値は2 nM、5 nM と 4 nMそれぞれに分かれます。StaurosporineはPKCδ(20 nM)とPKCε(73 nM)に作用することが弱くて、PKCζ (1086 nM)に対する活性も低いですが、他のキナーゼ(例えば、PKA、PKG、S6K、CaMKII等)に抑制活性を現れます。臨床3期。
ターゲット PKCα PKCγ PKCη PKCδ PKCε PKCζ
IC50 2 nM 5 nM 4 nM 20 nM 73 nM 1086 nM [1]

In vitro試験 Staurosporine, a microbial alkaloid, significantly inhibits protein kinase C from rat brain with IC50 of 2.7 nM. Staurosporine displays strong inhibitory effect against HeLa S3 cells with IC50 of 4 nM. [1] Staurosporine also inhibits a variety of other protein kinases, including PKA, PKG, phosphorylase kinase, S6 kinase, Myosin light chain kinase (MLCK), CAM PKII, cdc2, v-Src, Lyn, c-Fgr, and Syk with IC50 of 15 nM, 18 nM, 3 nM, 5 nM, 21 nM, 20 nM, 9 nM, 6 nM, 20 nM, 2 nM, and 16 nM, respectively. [2] Staurosporine (1 μM) induces >90% apoptosis in PC12 cells. Consistently, Staurosporine treatment induces a rapid and prolonged elevation of intracellular free calcium levels [Ca2+]i, accumulation of mitochondrial reactive oxygen species (ROS), and subsequent mitochondrial dysfunction. [3] The apoptosis of MCF7 cells induced by Staurosporine can be enhanced by the expression of functional caspase-3 via caspase-8 activation and Bid cleavage. [4] Staurosporine treatment at 1 μM only partially inhibits IL-3-stimulated Bcl2 phosphorylation but completely blocks PKC-mediated Bcl2 phosphorylation. [5] Staurosporine induces apoptosis of human foreskin fibroblasts AG-1518, depending on the lysosomal cathepsins D mediated cytochrome c release and caspase activation. [6] In addition to activating the classical mitochondrial apoptosis pathway, Staurosporine triggers a novel intrinsic apoptosis pathway, relying on the activation of caspase-9 in the absence of Apaf-1. [7]
In vivo試験 In the gerbil and rat ischemia models, Staurosporine pretreatment (0.1-10 ng) before ischemia prevents neuronal damage in a dose-dependent manner, suggesting the involvement of PKC in CAl pyramidal cell death after ischemia. [8]
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ:

[1]

Enzyme assay and binding assay Protein kinase C is assayed in a reaction mixture (0.25 mL) containing 5 μmol of Tris/HCl, pH 7.5, 2.5 μmol of magnesium acetate, 50 μg of histone II S, 20 μg of phosphatidylserine, 0.88 μg of diolein, 125 nmol of CaCl2, 1.25 nmol of [γ-32]ATP (5-10 × 104 cpm/nmol) and 5 μg of partially purified enzyme. The binding of [3H]PDBu to protein kinase C is determined: Reaction mixture (200 μL contained 4 μmo1 of Tris/malate, pH 6.8, 20 μmol of KCl, 30 nmol of CaC12, 20 μg of phosphatidylserine, 5 μg of partially purified protein kinase C, 0.5% (final concentration) of DMSO,10 pmol of [3H]PDBu (l-3 × 104 cpm/pmol) and 10 μL of various amounts of Staurosporine.

細胞アッセイ:

[3]

細胞株 PC12
濃度 Dissolved in DMSO, final concentration 1 μM
反応時間 ~32 hours
実験の流れ

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.

動物実験:

[8]

動物モデル Male Mongolian gerbils or male Wistar rats subjected to transient ischemia
製剤 Dissolved in DMSO, and diluted in saline
投薬量 ~10 ng
投与方法 Stereotaxically administered into the bilateral CAl subfield of the hippocampus

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Staurosporine SDF
分子量 466.53
化学式

C28H26N4O3

CAS No. 62996-74-1
保管 3年-20℃
2年-80℃in solvent
別名 CGP 41251
溶解度 (25°C) * In vitro DMSO 4 mg/mL (8.57 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 9,13-Epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one, 2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-11-(methylamino)-, [9S-(9α,10β,11β,13α)]-

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