G-963
G-963 is an allosteric inhibitor of mitogen-activated protein kinase kinase (MEK) with a MEK1 IC50 of 0.012 μM. G-963 interacts with Ser212 of MEK and exhibits potent antiproliferative activity against HCT116 colon cancer cells (EC50 = 0.120 μM) and A375 melanoma cells (EC50 = 0.025 μM). G-963 can be used for the research of colon cancer, melanoma.
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- CAS No.: 1009330-74-8
- 화학식: C16H13FIN3O4
- 분자량:457.19
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All MEK Isoforms
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Biological Activity
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MEK1 0.012 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | EC50 |
0.025 μM
Compound: G-963
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Antiproliferative activity against human A375 cells assessed as inhibition of cell proliferation after 72 hrs
Antiproliferative activity against human A375 cells assessed as inhibition of cell proliferation after 72 hrs
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[PMID: 25193232] |
G-963 inhibits MEK1 with an IC50 of 0.012 μM, inhibits proliferation of HCT116 colon cancer cells with an EC50 of 0.120 μM and A375 melanoma cells with an EC50 of 0.025 μM, and shows weak inhibition of cytochrome P450 enzymes 2C9, 2C19, 3A4, 2D6, and 1A2 with IC50 values > 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1009330-74-8
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분자량 457.19
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화학식 C16H13FIN3O4
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SMILES
O=C(C1=C(NC2=CC=C(C=C2F)I)C3=C(C=CN=C3)O1)NOCCO
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)