ERK2-IN-7
ERK2-IN-7 is an ATP-competitive ERK2 inhibitor (mouse IC50 = 0.36 μM (cERK2) and 2.6 μM (aERK2); Kd = 0.05 μM (apo ERK2) and 0.14 μM (pERK2)). ERK2-IN-7 binds both inactive and phosphorylated ERK2 and blocks MEK-mediated ERK1/2 phosphorylation through induced-fit conformational changes of the Gly-rich loop and Tyr34, thereby inhibiting p90RSK phosphorylation and proliferation in BRAF-mutant cancer cells. ERK2-IN-7 can be used for research on melanoma and colon cancer.
For research use only. We do not sell to patients.
- CAS No.: 947605-77-8
- Formula: C25H29ClN4O4
- Molecular Weight:484.98
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
ERK2 0.36 μM (IC50, inactive) |
ERK2 2.6 μM (IC50, active) |
ERK2 0.05 μM (Kd, apo ERK2) |
ERK2 0.14 μM (Kd, pERK2) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2058 | EC50 |
800 nM
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Inhibition of ERK1/2 phosphorylation in human A2058 BRAF-mutant melanoma cells after 4 hrs incubation measured by immunoblotting for phospho-ERK1,2 and total ERK1,2.
Inhibition of ERK1/2 phosphorylation in human A2058 BRAF-mutant melanoma cells after 4 hrs incubation measured by immunoblotting for phospho-ERK1,2 and total ERK1,2.
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25313996 |
| A2058 | IC50 |
28.8 μM
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Antiproliferative activity against human A2058 BRAF-mutant melanoma cells assessed as cell growth inhibition after 3 days incubation by CellTiter-Glo assay.
Antiproliferative activity against human A2058 BRAF-mutant melanoma cells assessed as cell growth inhibition after 3 days incubation by CellTiter-Glo assay.
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25313996 |
| A375-SM | IC50 |
11.5 μM
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Antiproliferative activity against human A375SM melanoma cells assessed as cell growth inhibition after 3 days incubation by CellTiter-Glo assay.
Antiproliferative activity against human A375SM melanoma cells assessed as cell growth inhibition after 3 days incubation by CellTiter-Glo assay.
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25313996 |
| COLO 205 | IC50 |
10.8 μM
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Antiproliferative activity against human Colo-205 colon cancer cells assessed as cell growth inhibition after 3 days incubation by CellTiter-Glo assay.
Antiproliferative activity against human Colo-205 colon cancer cells assessed as cell growth inhibition after 3 days incubation by CellTiter-Glo assay.
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25313996 |
In Vitro
ERK2-IN-7 (3 days) inhibits the proliferation of BRAF-mutant A2058, A375SM, and Colo-205 cells with IC50 values of 28.8, 11.5, and 10.8 μM, respectively, and shows > 100 μM in wild-type BRAF CHL-1 cells[1].
ERK2-IN-7 (15-100 μM) binds apo ERK2 with a Kd of 0.05 μM and pERK2 with a Kd of 0.14 μM[1].
ERK2-IN-7 binds ERK2 in an induced-fit mode at a resolution of 1.65 Å, with key hinge interactions and a new side pocket formed by conformational changes in the Gly-rich loop/Tyr34[1].
ERK2-IN-7 (1 µM) inhibits ERK2 (MAPK1) and ERK1 (MAPK3) activity by 47% and 54%, respectively, in kinase counter-screening[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A2058 BRAF-mutant melanoma cells
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Concentration:150, 312, 625, 1250, 2500, 5000, or 10000 nM
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Incubation Time:4 h at 37 °C
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Result:Inhibited phosphorylation of RSK and inhibited phosphorylation of ERK1,2 in a dose-dependent manner with an EC50 of ~800 nM.
Chemical Information
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CAS No. 947605-77-8
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Molecular Weight 484.98
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Formula C25H29ClN4O4
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SMILES
C(CN1C[C@H](C(NC2=CC(Cl)=C(O)C=C2)=O)CC1)(=O)N3CCN(CC3)C4=CC=C(C(C)=O)C=C4
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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)
ERK2-IN-7 Related Classifications
HY-12931 Related Classifications
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