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
제품 설명
IC50 & Target
[1]|
CK2 40.2 nM (IC50) |
In Vitro
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. Further protocols information, click here.
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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 |
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.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)