受注:045-509-1970 |
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Synonyms | GOE 6983, Gö 6983 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C26H26N4O3 |
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分子量 | 442.51 | CAS No. | 133053-19-7 | ||||
Solubility (25°C)* | 体外 | DMSO | 89 mg/mL (201.12 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) |
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* <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 | Go 6983 (GOE 6983, Gö 6983) is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ. |
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in vitro | Go 6983 (300 μM) suppresses PKCμ auto-phosphorylation by 20% reduction in NIH3T3 transfected with PKCμ. [1] In hearts reperfused with PMNs and Gö 6983 (100 nM), left ventricular developed pressure (LVDP) and the rate of LVDP recoveres to 89% and 74% of baseline values, respectively, significantly higher than PMNs alone. Gö 6983 (100 nM) significantly reduces PMNs adherence to the endothelium and infiltration into the myocardium compared with Ischemia followed by reperfusion (I/R)+ PMN hearts, and significantly inhibits superoxide release from PMNs by 90%. Gö 6983 attenuates post-I/R cardiac contractile dysfunction in the presence of PMNs, which may be related in part to decreased superoxide production. [2] Gö 6983 significantly inhibits antigen-induced superoxide release from leukocytes of patients previously sensitized to tree pollen. Go 6983 inhibited intracellular Ca(2+) accumulation in human vascular tissue, suggesting a mechanism for its vasodilator properties. [3] Go-6983 (1 μM) combined with Ro-31-8425 (390 nM) slightly inhibits Angiotensin II–induced PLD2 activity in PGSMCs. [4] Go 6983 is isoform-specific PKC inhibitor that target the ATP binding site. Go 6983 inhibits ΔPfPKB activity with an IC50 of 1 μM. In Go 6983 (5 μM)-treated cells, the number of rings in the following cycle is markedly less compared with the control cultures. Go 6983 (5 μM) treatment results in an almost 60% decrease in formation of new rings in P. falciparum cultures. [5] |
in vivo | Go6983 (22.0 μg/mouse, i.v.) strongly inhibits tumor metastasis by 51.2 % in a mouse pulmonary B16BL6 tumor model. [6] |
キナーゼアッセイ | Binding assay | |
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Phosphorylation reactions are carried out in a total volume of 100 μL, containing buffer C (50 mM Tris-HC1, pH 7.5, 10 mM β-mercaptoethanol), 4 mM MgCl2, 10 μg PS, 100 nM TPA, 5 μL of a Sf158 cell extract as a source of recombinant PKCμ or of Sf9 cell extracts as a source of other recombinant PKC isoenzymes, 10 μg of syntide 2 as substrate, and 35 μM ATP containing 1 μCi [γ-32P]ATP. In some experiments PS and TPA are omitted or various inhibitors at concentrations indicated in the text are added. After incubation for 10 min at 30℃, the reaction is terminated by transferring 50 μL of the assay mixture onto a 20 mm square piece of phosphocellulose paper, which is washed 3 times in deionized water and twice in acetone. The radioactivity on each paper is determined by liquid scintillation counting. | ||
細胞アッセイ | 細胞株 | Cell-free assays |
濃度 | IC50 of 7, 7, 6 and 10 nM for PKCα, PKCβ, PKCγ and PKCδ, respectively. | |
反応時間 | ||
実験の流れ | ||
動物実験 | 動物モデル | Mice bearing B16BL6 tumors |
投薬量 | 22 μg/mouse | |
投与方法 | i.v. |
Data from [Data independently produced by , , Amino Acids, 2016, 48(5):1185-97]
Data from [Data independently produced by , , Cellular Signalling, 2014, 26(11): 2436-2445]
Data from [Data independently produced by , , PLoS One, 2015, 10(4): e0122179 ]
High-throughput chemogenetic drug screening reveals PKC-RhoA/PKN as a targetable signaling vulnerability in GNAQ-driven uveal melanoma [ Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101244] | PubMed: 37858338 |
Alternative splicing of HDAC7 regulates its interaction with 14-3-3 proteins to alter histone marks and target gene expression [ Cell Rep, 2023, 42(3):112273] | PubMed: 36933216 |
PTH regulates osteogenesis and suppresses adipogenesis through Zfp467 in a feed-forward, PTH1R-cyclic AMP-dependent manner [ Elife, 2023, 12e83345] | PubMed: 37159501 |
The biased M3 mAChR ligand PD 102807 mediates qualitatively distinct signaling to regulate airway smooth muscle phenotype [ J Biol Chem, 2023, 299(10):105209] | PubMed: 37660916 |
Histamine promotes angiogenesis through a histamine H1 receptor-PKC-VEGF-mediated pathway in human endothelial cells [ J Pharmacol Sci, 2023, 151(4):177-186] | PubMed: 36925216 |
PKCβII phosphorylates ACSL4 to amplify lipid peroxidation to induce ferroptosis [ Nat Cell Biol, 2022, 24(1):88-98] | PubMed: 35027735 |
Alternative splicing of apoptosis genes promotes human T cell survival [ Elife, 2022, 11e80953] | PubMed: 36264057 |
Nucleosome remodeling and deacetylation complex and MBD3 influence mouse embryonic stem cell naïve pluripotency under inhibition of protein kinase C [ Cell Death Discov, 2022, 8(1):344] | PubMed: 35915078 |
Nucleosome remodeling and deacetylation complex and MBD3 influence mouse embryonic stem cell naïve pluripotency under inhibition of protein kinase C [ Cell Death Discov, 2022, 8(1):344] | PubMed: 35915078 |
LPIN1 Induces Gefitinib Resistance in EGFR Inhibitor-Resistant Non-Small Cell Lung Cancer Cells [ Cancers (Basel), 2022, 14(9)2222] | PubMed: 35565351 |
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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