受注:045-509-1970 |
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Synonyms | PD406976 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H18N4O |
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分子量 | 377.42 | CAS No. | 136194-77-9 | |
Solubility (25°C)* | 体外 | DMSO | 44.7 mg/mL warmed with 50ºC water bath (118.43 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 | Go6976 (PD406976) is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3. |
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in vitro | Go6976 have no effect on the kinase activity of the Ca(2+)-independent PKC subtypes delta, epsilon, and zeta. [1] Beside WT JAK2, Go6976 also inhibits the mutant forms (JAK2 V617F and TEL-JAK2) found in haematological malignancies, and has activity against mutant forms of FLT3. In AML cells, Go6976 reduces the survival to 55% of control in FLT3-ITD cases and to 69% in FLT3-WT samples.[2] Go 6976 potently inhibits HIV-1 induction by Bryostatin 1, tumor necrosis factor alpha, and interleukin 6. [3] |
in vivo | Go6976 (2.5 mg/kg i.p.), as a PKD inhibitor, effectively prevents LPS/D: -GalN-induced acute liver injury by inhibition of MAPKs activation to reduce TNF-α production, and significantly improves the survival of LPS/D-GalN-challenged mice. [4] |
キナーゼアッセイ | PKC Activity Assay | |
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In brief, for measuring PKCα, and PKCβ1 and PKC from rat brain, the assay mixture of 200 μl contains 50 mM HEPES (pH7.5), 5 mM MgCl2, 1 mM EDTA, 1.25 mM EGTA, 1.32 mM CaC12, 1 mM dithiothreitol, 1 μg of phosphatidylserine, 0.2 μg of diolein, 40 μg of histone Hi, 10 μM [γ-32P]ATP (1 μCi/ml), and 5-10 units (pmol of Pi/min) of PKC. Assays are started by the addition of [γ-32P]ATP, incubated for 5 min at 30 °C, stopped by the addition of 2 ml of 8.5% H3PO4, filtered through 0.45-μm nitrocellulose filters, and evaluated by scintillation counting. | ||
細胞アッセイ | 細胞株 | Primary AML cells |
濃度 | 1 μM | |
反応時間 | 48 hours | |
実験の流れ | Cells are suspended at 2 × 105 per point in 200 μl RPMI/10% FCS. The inhibitor under investigation is added at the appropriate concentration and the cells incubated for 48 h at 37°C, 5% CO2. MTS activity is measured by CellTiter kit according to the manufacturers instructions. Results are expressed as a percentage of control (cells without inhibitor). |
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動物実験 | 動物モデル | LPS/D-GalN-challenged mice |
投薬量 | 2.5 mg/kg | |
投与方法 | i.p. |
, , Cell Signal, 2016, 28(9):1422-31.
Data from [Data independently produced by , , Acta Physiol, 2018, 223(3):e13055]
Data from [Data independently produced by , , J Biol Chem, 2018, doi:10.1074/jbc.RA118.002191]
Lamin A/C phosphorylation at serine 22 is a conserved heat shock response to regulate nuclear adaptation during stress [ J Cell Sci, 2023, 136(4)jcs259788] | PubMed: 36695453 |
Spatially differential regulation of ATF2 phosphorylation contributes to warning coloration of gregarious locusts [ Sci Adv, 2023, 9(34):eadi5168] | PubMed: 37611100 |
Spatially differential regulation of ATF2 phosphorylation contributes to warning coloration of gregarious locusts [ Sci Adv, 2023, 9(34):eadi5168] | PubMed: 37611100 |
Trafficking of the glutamate transporter is impaired in LRRK2-related Parkinson's disease [ Acta Neuropathol, 2022, 144-1:81-106] | PubMed: 35596783 |
p52 signaling promotes cellular senescence [ Cell Biosci, 2022, 12(1):43] | PubMed: 35379326 |
(+)-Borneol inhibits the generation of reactive oxygen species and neutrophil extracellular traps induced by phorbol-12-myristate-13-acetate [ Front Pharmacol, 2022, 13:1023450] | PubMed: 36419617 |
Combination of IL-17A/F and TNF-α uniquely alters the bronchial epithelial cell proteome to enhance proteins that augment neutrophil migration [ J Inflamm (Lond, 2022, 19(1:26)] | PubMed: 36517803 |
Exploiting polypharmacology to dissect host kinases and kinase inhibitors that modulate endothelial barrier integrity [ Cell Chem Biol, 2021, S2451-9456(21)00303-2] | PubMed: 34216546 |
Ubash3b promotes TPA-mediated suppression of leukemogenesis through accelerated downregulation of PKCδ protein [ Biochimie, 2021, 184:8-17] | PubMed: 33556471 |
Five Constituents in Psoralea corylifolia L. Attenuate Palmitic Acid-Induced Hepatocyte Injury via Inhibiting the Protein Kinase C-α/Nicotinamide-Adenine Dinucleotide Phosphate Oxidase Pathway. [ Front Pharmacol, 2020, 10:1589] | PubMed: 32116659 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。