1. MAPK/ERK Pathway
  2. MEK
  3. G-963

G-963 是丝裂原活化蛋白激酶激酶 (MEK) 的变构抑制剂,对 MEK1IC50 为 0.012 μM。G-963 可与 MEK 的 Ser212 结合,对 HCT116 结肠癌细胞 (EC50 = 0.120 μM) 和 A375 黑色素瘤细胞 (EC50 = 0.025 μM) 表现出强效抗增殖活性。G-963 可用于结肠癌、黑色素瘤的研究。

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G-963

G-963 Chemical Structure

CAS No. : 1009330-74-8

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  • 参考文献

生物活性

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[1].

IC50 & Target[1]

MEK1

0.012 μM (IC50)

体外研究
(In Vitro)

G-963 对 MEK1 具有抑制作用,IC50 为 0.012 μM;对 HCT116 结肠癌细胞的增殖具有抑制作用,EC50 为 0.120 μM,对 A375 黑色素瘤细胞的增殖也具有抑制作用,EC50 为 0.025 μM;同时对细胞色素 P450 酶 2C9、2C19、3A4、2D6 和 1A2 仅表现出微弱抑制作用,其 IC50 值均 > 10 μM[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

457.19

Formula

C16H13FIN3O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
G-963
目录号:
HY-182538
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