中文同义词:
AS601245.TFA盐;JNK抑制剂(AS601245);ALPHA-[2-[[2-(3-吡啶基)乙基]氨基]-4-嘧啶基]-2-苯并噻唑乙腈
英文同义词:
2-(1,3-benzothiazol-2-yl)-2-[2-(2-pyridin-3-ylethylamino)pyrimidin-4-yl]acetonitrile;AS601245;AS601245.TFA;JNK Inhibitor V;alpha-[2-[[2-(3-Pyridinyl)ethyl]amino]-4-pyrimidinyl]-2-benzothiazoleacetonitrile;CS-1619;2-Benzothiazoleacetonitrile, α-[2-[[2-(3-pyridinyl)ethyl]amino]-4-pyrimidinyl]-
相关类别:
小分子抑制剂;小分子抑制剂，天然产物;细胞生物学试剂;Inhibitors
沸点
635.6±65.0 °C(Predicted)
密度
1.366±0.06 g/cm3(Predicted)
储存条件
Keep in dark place,Sealed in dry,Store in freezer, under -20°C
酸度系数(pKa)
5.32±0.10(Predicted)
生物活性
AS601245 是一种口服活性、选择性、ATP竞争性的 JNK 抑制剂，IC50 分别为 150、220和 70 nM，对三种 JNK 人类亚型 (hJNK1、hJNK2和hJNK3)。AS601245 对 c-src、CDK2 和 c-Raf 的选择性为 10-20 倍，对一系列 Ser/Thr 和 Tyr 蛋白激酶的选择性为 50-100 倍。具有神经保护特性。
靶点
hJNK1
150 nM (IC 50 )
hJNK2
220 nM (IC 50 )
hJNK3
70 nM (IC 50 )
hJNK1
150 nM (IC 50 )
hJNK2
220 nM (IC 50 )
体外研究
AS601245, an anti-Inflammatory JNK inhibitor, and Clofibrate have a synergistic effect in inducing cell responses and in affecting the gene expression profile in CaCo-2 colon cancer cells .
体内研究
AS601245 (40, 60, and 80 mg/kg; i.p.) provides significant protection against the delayed loss of hippocampal CA1 neurons in a gerbil model of transient global ischemia.
AS601245 (0.3-10 mg/kg; p.o.) is a potent inhibitor of LPS-induced TNF-α release in mice.
Animal Model: C3H/HEN mice
Dosage: 0.3, 1, 3, or 10 mg/kg
Administration: P.o.
Result: Decreased the TNF-α release in a dose-dependent manner.
Animal Model:
C3H/HEN mice
Dosage:
0.3, 1, 3, or 10 mg/kg
Result:
Decreased the TNF-α release in a dose-dependent manner.
