AKT-IN-28
AKT-IN-28 is an Akt allosteric inhibitor, a derivative of Shikonin (HY-N0822). AKT-IN-28 effectively binds to the allosteric site of Akt through hydrophobic and hydrogen interactions with Kd of 2.07 μM. AKT-IN-28 significantly inhibits Akt activity, induces cell apoptosis, arrests cell cycle in G2/M phase, and suppresses proliferation, migration and metabolism of KRAS mutant colorectal cancer cells.
For research use only. We do not sell to patients.
- CAS No.: 3099809-16-9
- Formula: C32H28FNO8
- Molecular Weight:573.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Caspase Isoforms
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Biological Activity
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Caspase 3 |
PARP |
Akt 2.07 μM (Kd) |
AKT-IN-28 (Compound L8) has a potent anti-proliferative activity (IC50 s of 4.51, 4.57, 5.07, 8.94 and 6.59 μM for HCT-8, HCT-116, PC-3, MDA-MB-231, and HeLa cells, respectively), with low cytotoxicity in normal cells (IC50 s of > 100 and 67 μM for MCF-10A and HCoEpiC cells)[1].
AKT-IN-28 (1-4 μM, 24 h) dose-dependently decreases the Akt enzyme activity, and significantly inhibits the total Akt, p-Akt, PARP and β-catenin protein expression, cell proliferation activity and migration, while increase of cleaved-PARP protein level in HCT-8 and HCT-116 cells[1].
AKT-IN-28 (0.25-1 μM, 7 days) significantly inhibites the viability of colon cancer cells with reduction of colony formation of HCT-116 cells[1].
AKT-IN-28 (2-8 μM, 24 h) effectively induces cell apoptosis and arrests cell cycle in G2/M phase (8 μM) with decrease of cycle-related proteins CDH1, CDK1, and CDC20, and increases caspase3 activity in HCT-116 and HCT-8 cells[1].
AKT-IN-28 (2-8 μM, 2-24 h) significantly reduces the glucose consumption, lactate production, and ATP level in HCT-116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 cells
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Concentration:1, 2, 4 μM
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Incubation Time:24 h
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Result:Significantly reduced the percentage of EdU-positive cells.
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Cell Line:HCT-8 cells, HCT-116 cells
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Concentration:1, 2, 4 μM
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Incubation Time:3, 6, 12, 24 h
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Result:Significantly reduced the number of metastasis colon cancer cells and enlarged the space area of migrating cells.
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Cell Line:HCT-116 cells
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Concentration:1, 2, 4 μM
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Incubation Time:24 h
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Result:Significantly inhibited the total Akt, p-Akt, PARP and β-catenin protein expression but increased cleaved-PARP protein level.
Obviously decreased the expression levels of cycle-related proteins CDH1, CDK1, and CDC20.
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Cell Line:HCT-8 cells, HCT-116 cells
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Concentration:2, 4, 8 μM
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Incubation Time:24 h
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Result:Arrested the cell cycle at G2/M phase at 8 μM in HCT-8 and HCT-116 cells.
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Cell Line:HCT-8 cells, HCT-116 cells
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Concentration:2, 4, 8 μM
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Incubation Time:24 h
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Result:Effectively induced cell apoptosis in HCT-8 and HCT-116 cells.
Chemical Information
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CAS No. 3099809-16-9
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Molecular Weight 573.57
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Formula C32H28FNO8
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SMILES
O=C1C2=C(O)C=CC(O)=C2C(C=C1[C@@H](C/C=C(C)\C)OC(CC3=CC=C(C=C3)NC(COC4=CC=C(C=C4)F)=O)=O)=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)