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  3. 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.

For research use only. We do not sell to patients.

GO847

GO847 Chemical Structure

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Description

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[1].

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.

Cell Proliferation Assay[1]

Cell Line: mouse AML C1498 cells, human AML THP-1 cells
Concentration: 0-20 μM
Incubation Time: 48 h
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.

Western Blot Analysis[1]

Cell Line: mouse AML C1498 cells, human AML THP-1 cells
Concentration: 0.9-8 μM
Incubation Time: 24 h
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
Molecular Weight

461.96

Formula

C21H24ClN5O3S

SMILES

COC1=CC(/C=N/N2C(SC)=NN=C2C3=CC=C(C=C3)OCCN(C)C)=C(C=C1O)Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
GO847
Cat. No.:
HY-183265
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