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Cat. No.: HY-182538

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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
Formule: C₁₆H₁₃FIN₃O₄
Masse moléculaire:457.19

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Please store the product under the recommended conditions in the Certificate of Analysis.

G-963 Chemical Structure

CAS No.: 1009330-74-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
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Activité biologique

Description

IC₅₀ & Target^[1]

MEK1

0.012 μM (IC₅₀)

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Cellular Effect

Cell Line	Type	Value	Description	References
A-375	EC₅₀	0.025 μM Compound: G-963	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	[PMID: 25193232]

In Vitro

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

CAS No. 1009330-74-8
Masse moléculaire 457.19
Formule C₁₆H₁₃FIN₃O₄
SMILES

O=C(C1=C(NC2=CC=C(C=C2F)I)C3=C(C=CN=C3)O1)NOCCO
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Robarge KD, et al. Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. Bioorg Med Chem Lett. 2014;24(19):4714-4723. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références

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G-963

Voir tous les produits spécifiques à Isoform MEK

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

G-963 Related Classifications

HY-182538 Related Classifications