GO847
GO847 is an orally active casein kinase 2 (CK2) inhibitor with an IC50 of 40.2 nM. GO847 increases intracellular ATP levels, impairs Mitochondrial metabolic flexibility, and promotes excessive mitochondrial ROS production. GO847 alters the period length of cellular circadian rhythms. GO847 inhibits the growth of acute myeloid leukemia cells. GO847 can be used for the research of acute myeloid leukemia.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C21H24ClN5O3S
- 分子量:461.96
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
CK2 40.2 nM (IC50) |
体外実験
GO847 (1×10-11-1×10-6 M) potently inhibits CK2 enzymatic activity in vitro with an IC50 of 40.2 nM[1].
GO847 (0-20 μM; 48 h) dose-dependently inhibits the growth of mouse AML C1498 cells (IC50 = 5.1 μM) and human AML THP-1 cells (IC50 = 1.7 μM) after 48 h of treatment[1].
GO847 (0.9-8 μM; 24 h) dose-dependently inhibits cellular CK2 activity in mouse AML C1498 cells and human AML THP-1 cells after 24 h of treatment, reducing phosphorylation of CK2 substrates including AKT1(S129)[1].
GO847 (5 μM; 24 h) impairs mitochondrial metabolic flexibility in mouse AML C1498 cells after 24 h of treatment, reducing spare respiratory capacity and abolishing glycolytic compensation in response to mitochondrial inhibition[1].
GO847 increases ATP levels, elevates mitochondrial membrane potential, and promotes excessive mitochondrial ROS production in mouse AML C1498 cells after 24 h of treatment with 5 μM GO847[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:mouse AML C1498 cells, human AML THP-1 cells
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Concentration:0-20 μM
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Incubation Time:48 h
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Result:Inhibited proliferation of both cell lines in a dose-dependent manner, with an IC50 of 5.1 μM for C1498 cells and 1.7 μM for THP-1 cells.
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Cell Line:mouse AML C1498 cells, human AML THP-1 cells
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Concentration:0.9-8 μM
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Incubation Time:24 h
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Result:Caused a dose-dependent reduction in phosphorylation signals of CK2 substrates, including AKT1 (S129), in both C1498 and THP-1 cells.
Showed slightly less potent activity compared to GO289.
Parmacokinetics
| Species | Dose | Route | Cmax | AUC0-t | T1/2 |
|---|---|---|---|---|---|
| Mice[1] | 100 mg/kg | i.p. | 0.5 μM | 4.0 μM·h | 7.4 h |
化学情報
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分子量 461.96
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分子式 C21H24ClN5O3S
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SMILES
COC1=CC(/C=N/N2C(SC)=NN=C2C3=CC=C(C=C3)OCCN(C)C)=C(C=C1O)Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
ホットトピック
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All
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Topics
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Most Recent
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Oldest
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Topics Circadian Rhythms & Cardiovascular Health
Circadian rhythms are endogenous ~24-hour timing systems that coordinate sleep-wake cycles, metabolism, endocrine signaling, and cardiovascular physiology.
2026-06-18
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)