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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.

For research use only. We do not sell to patients.

CAS No.: 1009330-74-8
Formula: C₁₆H₁₃FIN₃O₄
Molecular Weight:457.19

Storage:

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

MEK1

0.012 μM (IC₅₀)

All MEK Isoforms :

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
Molecular Weight 457.19
Formula C₁₆H₁₃FIN₃O₄
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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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Help & FAQs

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.

Keywords

100 mg

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