Staurosporine (STS)

製品コードS1421 バッチS142109

印刷

化学情報

Chemical Structure Synonyms AM-2282，Antibiotic AM-2282 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C28H26N4O3
分子量 466.53 CAS No. 62996-74-1
Solubility (25°C)* 体外 DMSO 93 mg/mL (199.34 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 5.000mg/ml (10.72mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 スタウロスポリン (Staurosporine (AM-2282、Antiviotic AM-2282、STS)) は、PKCα、PKCγ、および PKCη に対する強力な PKC 阻害剤であり、IC50 は 2 nM、5 nM、および 4 nM です。 無細胞アッセイでは、PKCδ (20 nM)、PKCε (73 nM) に対して効力が低く、PKCζ (1086 nM) に対してほとんど活性がありません。 また、PKA、PKG、S6K、CaMKII などの他のキナーゼに対しても阻害活性を示します。臨床フェーズ3。
in vitro Staurosporine (STS), a microbial alkaloid, significantly inhibits protein kinase C from rat brain with IC50 of 2.7 nM. It displays strong inhibitory effect against HeLa S3 cells with IC50 of 4 nM. [1] This compound 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] At 1 μM, it induces >90% apoptosis in PC12 cells. Consistently, such 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 STS can be enhanced by the expression of functional caspase-3 via caspase-8 activation and Bid cleavage. [4] Treatment at 1 μM only partially inhibits IL-3-stimulated Bcl2 phosphorylation but completely blocks PKC-mediated Bcl2 phosphorylation. [5] It 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, it triggers a novel intrinsic apoptosis pathway, relying on the activation of caspase-9 in the absence of Apaf-1. [7]
in vivo In the gerbil and rat ischemia models, pretreatment with Staurosporine (STS) (0.1–10 ng) before ischemia prevents neuronal damage in a dose-dependent manner, suggesting the involvement of PKC in CA1 pyramidal cell death after ischemia. [8]

プロトコル(参考用のみ)

キナーゼアッセイ 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 (STS).
細胞アッセイ 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 (STS) for ~32 hours, fixed in 4% paraformaldehyde, and stained with the DNA-binding dye Hoechst 33342. After visualization under epifluorescence illumination, the percentage of apoptotic cells (cells with condensed and fragmented DNA) is determined.
動物実験 動物モデル Male Mongolian gerbils or male Wistar rats subjected to transient ischemia
投薬量 ~10 ng
投与方法 Stereotaxically administered into the bilateral CAl subfield of the hippocampus

参考

  • https://pubmed.ncbi.nlm.nih.gov/3457562/
  • https://pubmed.ncbi.nlm.nih.gov/8529658/
  • https://pubmed.ncbi.nlm.nih.gov/9486765/
  • https://pubmed.ncbi.nlm.nih.gov/10734071/
  • https://pubmed.ncbi.nlm.nih.gov/10677502/
  • https://pubmed.ncbi.nlm.nih.gov/14576777/
  • https://pubmed.ncbi.nlm.nih.gov/21659556/
  • https://pubmed.ncbi.nlm.nih.gov/2384538/

カスタマーフィードバック

Data from [J Biomol Screen, 2013, 18(4), 388-99]

Data from [J Biomol Screen, 2013, 18(4), 388-99]

Data from [Data independently produced by PLoS One, 2012, 7(6), e39679]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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