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Synonyms | AM-2282,Antibiotic AM-2282 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C28H26N4O3 |
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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 | |||
* <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. |
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。 |
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in vitro | 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 | 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] |
キナーゼアッセイ | Enzyme assay and binding assay | |
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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 | 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. |
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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 |
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]
Design-rules for stapled peptides with in vivo activity and their application to Mdm2/X antagonists [ Nat Commun, 2024, 15(1):489] | PubMed: 38216578 |
Kisspeptin-10 binding to Gpr54 in osteoclasts prevents bone loss by activating Dusp18-mediated dephosphorylation of Src [ Nat Commun, 2024, 15(1):1300] | PubMed: 38346942 |
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics [ Mol Syst Biol, 2024, 20(1):28-55] | PubMed: 38177929 |
SUMOylation controls Hu antigen R posttranscriptional activity in liver cancer [ Cell Rep, 2024, 43(3):113924] | PubMed: 38507413 |
Identification and characterization of a potent and selective HUNK inhibitor for treatment of HER2+ breast cancer [ Cell Chem Biol, 2024, S2451-9456(24)00037-0] | PubMed: 38307028 |
The molecular basis of Abelson kinase regulation by its αI-helix [ Elife, 2024, 12RP92324] | PubMed: 38588001 |
Comparison of the oncolytic activity of a replication-competent and a replication-deficient herpes simplex virus 1 [ Immunology, 2024, 10.1111/imm.13775] | PubMed: 38444199 |
The efficacy of ferroptosis-inducing compounds IKE and RSL3 correlates with the expression of ferroptotic pathway regulators CD71 and SLC7A11 in biliary tract cancer cells [ PLoS One, 2024, 19(4):e0302050] | PubMed: 38603713 |
miR-10b-5p promotes tumor growth by regulating cell metabolism in liver cancer via targeting SLC38A2 [ Cancer Biol Ther, 2024, 25(1):2315651] | PubMed: 38390840 |
Lytic bacteriophages interact with respiratory epithelial cells and induce the secretion of antiviral and proinflammatory cytokines [ bioRxiv, 2024, 2024.02.06.579115] | PubMed: 38370761 |
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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