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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- 화학식: C21H24ClN5O3S
- 분자량:461.96
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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CK2 40.2 nM (IC50) |
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.
| 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 |
Chemical Information
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분자량 461.96
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)