SIK-IN-6
SIK-IN-6 is a selective SIK3 inhibitor with an IC50 of 15 nM. SIK-IN-6 exerts anticancer activity in acute myeloid leukemia with high MEF2C expression, but does not exhibit significant anticancer activity in acute myeloid leukemia with low MEF2C expression or in ovarian cancer. SIK-IN-6 can be used for the research of acute myeloid leukemia.
For research use only. We do not sell to patients.
- Formula: C26H24F2N4O3
- Molecular Weight:478.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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SIK3 15 nM (IC50) |
SIK1 130 nM (IC50) |
SIK2 200 nM (IC50) |
SIK-IN-6 (Compound 39) potently inhibits purified SIK3 with an IC50 of 15 nM, and shows weaker inhibition of purified SIK1 (IC50 130 nM) and SIK2 (IC50 200 nM), along with favorable in vitro ADME properties[1].
SIK-IN-6 (0.001-100 μM; 4 days) induces cytotoxicity in MEF2C-high MOLM13 AML cells with a GI50 of 1500 nM[1].
SIK-IN-6 (0.001-100 μM; 3 days) selectively induces cytotoxicity in MEF2C-high MV4-11 AML cells with a GI50 of 1200 nM, while sparing MEF2C-low U-937 AML cells and noncancerous HEK-293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM13 (MEF2C-high AML) cells
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Concentration:0.001-100 μM
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Incubation Time:4 days
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Result:Induced cytotoxicity with a GI50 of 1500 nM.
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Cell Line:MV4-11 (MEF2C-high AML), U-937 (MEF2C-low AML), and HEK-293 (noncancerous) cells
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Concentration:0.001-100 μM
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Incubation Time:3 days
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Result:Induced cytotoxicity in MV4-11 cells with a GI50 of 1200 nM.
Showed no significant cytotoxicity in U-937 cells (GI50 29000 nM).
Showed no significant cytotoxicity in HEK-293 cells (GI50 >30000 nM).
Chemical Information
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Molecular Weight 478.49
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Formula C26H24F2N4O3
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SMILES
COC1=CC(C2=CN=C3N2C=CC(C4=CC(C)=NC(C)=C4)=C3)=CC(OC)=C1C(N5CC(F)(C5)F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)