中文名称:

T5601640

中文同义词:

LIMK2抑制剂(T56-LIMKI);化合物T56-LIMKI

英文名称:

T5601640

英文同义词:

T5601640;T56-LIMKi;3-methyl-N-[3-[[3-(trifluoromethyl)phenyl]carbamoyl]phenyl]-1,2-oxazole-5-carboxamide;T-5601640(T56-LIMKi);3-Methyl-N-[3-[[[3-(trifluoromethyl)phenyl]amino]carbonyl]phenyl]-5-isoxazolecarboxamide;T5601640;T 5601640;T56-LIMKI;T56-LIMKi - T5601640;5-Isoxazolecarboxamide, 3-methyl-N-[3-[[[3-(trifluoromethyl)phenyl]amino]carbonyl]phenyl]-

CAS号:

924473-59-6

分子式:

C19H14F3N3O3

分子量:

389.33

EINECS号:

604-604-1

相关类别:

细胞生物学试剂

Mol文件:

924473-59-6.mol

沸点 

403.4±45.0 °C(Predicted)

密度 

1.426±0.06 g/cm3(Predicted)

储存条件 

2-8°C

形态

powder

酸度系数(pKa)

11.41±0.70(Predicted)

颜色

white to beige

生物活性

T56-LIMKi是LIM kinase 2 (LIMK2)抑制剂，抑制LIMK2介导的丝切蛋白磷酸化。

靶点

Target Value LIMK2 ()

Target

Value

LIMK2 ()

体外研究

T56-LIMKi efficiently inhibits the growth of ST88-14, U87, Panc-1 cells, A549 lung cancer cells with IC 50 values of 18.3, 7.4, 35.2 and 90 μM, respectively. T56-LIMKi decreases phosphorylated cofilin (p-cofilin) levels and thus inhibits growth of several cancerous cell lines, including those of pancreatic cancer, glioma and schwannoma. It blocks the phosphorylation of cofilin which leads to actin severance and inhibition of tumor cell migration, tumor cell growth, and anchorage-independent colony formation in soft agar. T56-LIMKi (10-50 μM) reduces p-cofilin in a dose-dependent manner in NF1 −/− MEFs with an IC 50 of 30 μM. Notably, the inhibitor does not affect the amounts of total cofil. 50μM T56-LIMKi causes a statistically significant reduction in the number of cells exhibiting stress fibers.

体内研究

T56-LIMKi can induce inhibition of cofilin phosphorylation and Panc-1 tumor shrinkage in vivo . Mice treated with T56-LIMKi (60 mg/kg) shows a significant decrease in tumor volume compared to control.

危险品运输编号 

UN 2811 6.1 / PGIII