| CAS |
No.924473-59-6 |
| 英文名称 |
T56-LIMKi |
| 别名 |
T5601640 |
| 分子式 |
C19H14F3N3O3 |
| 分子量 |
389.33 |
| 溶解性 |
Soluble in DMSO(Need ultrasonic) |
| 纯度 |
≥98% |
| 外观(性状) |
Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD08495674 |
| SMILES |
CC1=NOC(=C1)C(=O)NC2=CC=CC(=C2)C(=O)NC3=CC=CC(=C3)C(F)(F)F |
| InChIKey |
XVOKFRPKSAWELK-UHFFFAOYSA-N |
| InChI |
InChI=1S/C19H14F3N3O3/c1-11-8-16(28-25-11)18(27)24-14-6-2-4-12(9-14)17(26)23-15-7-3-5-13(10-15)19(20，21)22/h2-10H，1H3，(H，23，26)(H，24，27) |
| PubChem CID |
9438169 |
| 靶点 |
LIM Kinase (LIMK2) |
| 通路 |
Cytoskeleton |
| 背景说明 |
T56-LIMKi是选择性的LIMK2抑制剂。 |
| 生物活性 |
T56-LIMKi is a selective inhibitor of LIMK2; inhibits the growth of Panc-1 cells with an IC50 of 35.2 μM.[1-2] |
| In Vitro |
T56-LIMKi efficiently inhibits the growth of ST88-14， U87， Panc-1 cells， A549 lung cancer cells with IC50 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[1]. 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 IC50 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[2]. |
| In Vivo |
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[1]. |
| 细胞实验 |
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[1]. |
| 动物实验 |
Mice: T56-LIMKi is dissolved in 0.5% carboxymethylcellulose solution. Mice are implanted with xenografted Panc-1 cells. Treatment is started 7 days later. Mice in the two experimental groups are each treated with a daily oral non-toxic dose of T56-LIMKi (30 or 60 mg/kg in gavage) and mice in the control group receives only the vehicle (0.5% CMC) in the gavage[1]. |
| 数据来源文献 |
[1]. Rak R， et al. Novel LIMK2 Inhibitor Blocks Panc-1 Tumor Growth in a mouse xenograft model. Oncoscience. 2014 Jan 1;1(1):39-48. eCollection 2014.
[2]. Mashiach-Farkash E， et al. Computer-based identification of a novel LIMK1/2 inhibitor that synergizes with salirasib to destabilize the actin cytoskeleton. Oncotarget. 2012 Jun;3(6):629-39. |
| 规格 |
1mg 5mg 10mg 25mg 50mg 100mg |
| 单位 |
瓶 |
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