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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1009330-74-8
- 分子式: C16H13FIN3O4
- 分子量:457.19
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
MEK アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
[1]|
MEK1 0.012 μM (IC50) |
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] |
体外実験
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.
化学情報
-
CAS 番号 1009330-74-8
-
分子量 457.19
-
分子式 C16H13FIN3O4
-
SMILES
O=C(C1=C(NC2=CC=C(C=C2F)I)C3=C(C=CN=C3)O1)NOCCO
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)