首页 MAPK MNK CGP 57380
CGP 57380
编号 T6440     别名: MNK1 Inhibitor, MNK1 Inhibitor
CAS 522629-08-9     分子式 C11H9FN6     分子量 244.23
靶点: MNK1;
CGP 57380 is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases.
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规格 库存 单价 数量
1 mg 上海现货 265.00
5 mg 上海现货 828.00
10 mg 上海现货 1240.00
50 mg 上海现货 5155.00
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生物活性

产品描述

CGP 57380 is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases.

靶点活性

MNK1,2.2μM

体外活性

CGP57380 inhibits phosphorylation of eIF4E in cellular assays with IC50 of about 3 μM. CGP57380 causes dephosphorylation of eIF4E, and induces a further increase in the cap-dependent reporter in 293 cells. [1] CGP57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy. [2] CGP57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs). [3] CGP57380 prevents the serial replating function of BC progenitors. [4]

体内活性

CGP57380 (40 mg/kg/d i.p.) potently extinguishes the ability of BC CML cells to serially transplant-immunodeficient mice and function as LSCs. [4]

激酶实验

Recombinant p38 isoforms are activated by Mkk6(E) under the following conditions: p38 (100 ng/mL), Mkk6(E) (30 ng/mL), ATP (100 mM) are mixed in kinase buffer (25 mM Hepes, 25 mM b-glycerophosphate, 0.1 mM sodium orthovanadate, 25 mM MgCl2, 2.5 mM DTT, pH 7.4) and incubated for 30 min at 30°C. A typical assay reaction for Mnk1 activity contained Mnk1 (2 ng/mL), HA-eIF4E (10 ng/mL), ATP (300 mM) in kinase buffer. The reaction is started by addition of activated p38 (0.03-3 ng/mL) and stopped after 30 min at 30°C by addition of SDS loading buffer. Inhibitors of Mnk1 are identified under the same assay conditions, except that Mnk1 is pre-activated using active p38a before exposure to the substrate and inhibitors.

动物实验

动物模型:mice (n=5 mice

化学信息

分子量

244.23

分子式

C11H9FN6

CAS

522629-08-9

溶解度

DMSO: 45 mg/mL (184.3 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 4.095 ml 20.473 ml 40.945 ml
5 mM 0.819 ml 4.095 ml 8.189 ml
10 mM 0.409 ml 2.047 ml 4.095 ml
50 mM 0.082 ml 0.409 ml 0.819 ml
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本产品收录于以下化合物库中:
  • 经典已知活性库
  • 抗癌化合物库
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