Go 6976

製品コードS7119 バッチS711902

印刷

化学情報

Chemical Structure Synonyms PD406976 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H18N4O
分子量 377.42 CAS No. 136194-77-9
Solubility (25°C)* 体外 DMSO 44.7 mg/mL (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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Go6976 (PD406976) は、PKC (ラット脳) に対して7.9 nM、PKCα に対して2.3 nM、PKCβ1 に対して6.2 nM のIC50 値を示す強力なPKC阻害剤です。また、JAK2 および Flt3 の強力な阻害剤でもあります。
in vitro Go6976 have no effect on the kinase activity of the Ca(2+)-independent PKC subtypes delta, epsilon, and zeta. Beside WT JAK2, this compound 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, this chemical reduces the survival to 55% of control in FLT3-ITD cases and to 69% in FLT3-WT samples. It potently inhibits HIV-1 induction by Bryostatin 1, tumor necrosis factor alpha, and interleukin 6.
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.

プロトコル(参考用のみ)

キナーゼアッセイ PKC Activity Assay
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 this compound).
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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/8486620/
  • https://pubmed.ncbi.nlm.nih.gov/16956345/
  • https://pubmed.ncbi.nlm.nih.gov/7685108/
  • https://pubmed.ncbi.nlm.nih.gov/21063746/

カスタマーフィードバック

, , 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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Elevated Sphingosine Levels Suppress Profibrotic TGF-β Signaling via the PKC/miR-21/SMAD7 Axis in Sphingosine Kinase 2-Deficient Renal Fibroblasts and Unilateral Ureteral Obstruction-Induced Kidney Fibrosis [ FASEB J, 2025, 39(12):e70768] PubMed: 40558859
LRRC8A-containing anion channels promote glioblastoma proliferation via a WNK1/mTORC2-dependent mechanism [ bioRxiv, 2025, 2025.02.02.636139] PubMed: 39975357
PKCα Induced the Generation of Extracellular Vesicles in Activated Platelets to Promote Breast Cancer Metastasis [ Int J Biol Sci, 2024, 20(10):3956-3971] PubMed: 39113702
G-CSFR-induced leukocyte transendothelial migration during the inflammatory response is regulated by the ICAM1-PKCa axis: based on multiomics integration analysis [ Cell Biol Toxicol, 2024, 40(1):90] PubMed: 39433604
A role for plasma membrane Ca2+ ATPases in regulation of cellular Ca2+ homeostasis by sphingosine kinase-1 [ Pflugers Arch, 2024, 476(12):1895-1911.] PubMed: 39392480
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
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

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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