AKT-IN-30
AKT-IN-30 is an Akt inhibitor. AKT-IN-30 shows IC50 values of 25 nM, 1264 nM, and 8205 nM against human Akt3, Akt2, and Akt1, respectively, demonstrating selectivity for the Akt3 isoform. AKT-IN-30 exhibits moderate intrinsic thiol reactivity toward glutathione. AKT-IN-30 shows antiproliferative activity in breast cancer cell lines. AKT-IN-30 can be used for research on breast cancer.
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- Formule: C44H49N7O4
- Masse moléculaire:739.90
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
Akt3 25 nM (IC50) |
Akt2 1264 nM (IC50) |
Akt1/PKBα 8205 nM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
1184 nM
|
Cellular target engagement against NanoLuc-Akt1 in HEK293 cells assessed by NanoBRET assay using 0.5 μM tracer K10 incubated 3 hrs.
Cellular target engagement against NanoLuc-Akt1 in HEK293 cells assessed by NanoBRET assay using 0.5 μM tracer K10 incubated 3 hrs.
|
42808171 |
| HEK293 | EC50 |
353 nM
|
Cellular target engagement against NanoLuc-Akt2 in HEK293 cells assessed by NanoBRET assay using 0.5 μM tracer K10 incubated 3 hrs.
Cellular target engagement against NanoLuc-Akt2 in HEK293 cells assessed by NanoBRET assay using 0.5 μM tracer K10 incubated 3 hrs.
|
42808171 |
| HEK293 | EC50 |
35 nM
|
Cellular target engagement against NanoLuc-Akt3 in HEK293 cells assessed by NanoBRET assay using 0.5 μM tracer K10 incubated 3 hrs.
Cellular target engagement against NanoLuc-Akt3 in HEK293 cells assessed by NanoBRET assay using 0.5 μM tracer K10 incubated 3 hrs.
|
42808171 |
| ZR-75-1 | EC50 |
1189 nM
|
Antiproliferative activity against ZR-75-1 cells assessed as viability reduction by CellTiter-Glo luminescence assay measured on day 5.
Antiproliferative activity against ZR-75-1 cells assessed as viability reduction by CellTiter-Glo luminescence assay measured on day 5.
|
42808171 |
| MDA-MB-468 | EC50 |
6706 nM
|
Antiproliferative activity against MDA-MB-468 cells assessed as viability reduction by CellTiter-Glo luminescence assay measured on day 5.
Antiproliferative activity against MDA-MB-468 cells assessed as viability reduction by CellTiter-Glo luminescence assay measured on day 5.
|
42808171 |
In Vitro
AKT-IN-30 binds Akt3 with an EC50 of 35 nM in HEK293 cells and shows selectivity for Akt3 over Akt1 and Akt2[1].
AKT-IN-30 inhibits Akt3 with an HTRF IC50 of 25 nM, showing 327-fold and 50-fold selectivity over Akt1 and Akt2, respectively[1].
The GSH t1/2 of AKT-IN-30 is 213 min, indicating that it has moderate intrinsic thiol reactivity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Masse moléculaire 739.90
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Formule C44H49N7O4
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SMILES
O=C(C=C)NC1=CC2=C(C=C1)NC(N2C(CC3)CCN3CC(C=C4)=CC=C4C5=NC=C(NC(C[C@H]6CC[C@H](N(C)C(C)=O)CC6)=O)C=C5C7=CC=CC=C7)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)