GNE-4997
GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity.
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: 1705602-02-3
- 分子式: C25H27F2N5O3S
- 分子量:515.58
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
Ki: 0.09 nM (ITK)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Hepatocyte | IC50 |
>100 μM
Compound: 28, GNE-4997
|
Cytotoxicity against hepatocytes (unknown origin)
Cytotoxicity against hepatocytes (unknown origin)
|
[PMID: 25844760] |
| Jurkat | IC50 |
0.004 μM
Compound: 28, GNE-4997
|
Inhibition of ITK in TCR stimulated human Jurkat T cells assessed as reduction of PLC-gamma phosphorylation preincubated for 30 mins followed by TCR induction for 2 mins
Inhibition of ITK in TCR stimulated human Jurkat T cells assessed as reduction of PLC-gamma phosphorylation preincubated for 30 mins followed by TCR induction for 2 mins
|
[PMID: 25844760] |
| Jurkat | IC50 |
12 μM
Compound: 28, GNE-4997
|
Cytotoxicity against human Jurkat T cells without TCR stimulation assessed as cell viability by ATPlite assay
Cytotoxicity against human Jurkat T cells without TCR stimulation assessed as cell viability by ATPlite assay
|
[PMID: 25844760] |
GNE-4997 inhibits PLC-γ phosphorylation in Jurkat cells by T-cell receptor stimulation with an IC50 of 4 nM [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
-
CAS 番号 1705602-02-3
-
分子量 515.58
-
分子式 C25H27F2N5O3S
-
SMILES
O=C(C1=NNC2=C1C[C@H](C3(F)F)[C@@]3(C)C2)NC4=CN([C@H](C5=CC=CC=C5)[C@@H]6S(CCCC6)(=O)=O)N=C4
-
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)