R-10015

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Chemical Structure| 2097938-51-5 同义名 : -
CAS号 : 2097938-51-5
货号 : A1177091
分子式 : C20H19ClN6O2
纯度 : 99%+
分子量 : 410.857
MDL号 : MFCD32067935
存储条件：

Pure form Keep in dark place,Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(146.04 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 LIM kinase (LIMK) plays a critical role in orchestrating dendritic actin dynamics during memory processing, since it is the convergent downstream target of both the Rac1/PAK and RhoA/ROCK pathways that in turn induce cofilin phosphorylation and prevent depolymerization of actin filaments[2]. LIMK-1 signaling is important in vivo in the regulation of the actin cytoskeleton, spine morphology, and synaptic function, including hippocampal long-term potentiation (LTP), a prominent form of long lasting synaptic plasticity thought to be critical to memory formation[3].The protein expression of cofilin and LIMK was significantly decreased in thoracic aortic dissection tissue compared with normal control, (p = 0.004 for cofilin, p < 0.001 for LIMK). The mRNA levels of cofilin and LIMK were lower in thoracic aortic dissection than normal control and were coincident with the protein expression (p = 0.0039 for cofilin, p = 0.017 for LIMK). A significant correlation (Spearman's rho = -0.521, p = 0.019) was found between LIMK protein expression and maximal aortic diameter; lower levels of LIMK expression were associated with larger aortic diameters[4].R10015 as a lead compound that blocks LIMK activity by binding to the ATP-binding pocket. R10015 specifically blocks viral DNA synthesis, nuclear migration, and virion release. In addition, R10015 inhibits multiple viruses, including Zaire ebolavirus (EBOV), Rift Valley fever virus (RVFV), Venezuelan equine encephalitis virus (VEEV), and herpes simplex virus 1 (HSV-1), suggesting that LIMK inhibitors could be developed as a new class of broad-spectrum antiviral drugs{{Yi F, et al. Discovery of Novel Small-Molecule Inhibitors of LIM Domain Kinase for Inhibiting HIV-1. J Virol. 2017 Jun 9;91(13). pii: e02418-16.| https://pubmed.ncbi.nlm.nih.gov/28381571/}.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.43mL

0.49mL

0.24mL

12.17mL

2.43mL

1.22mL

24.34mL

4.87mL

2.43mL
参考文献

[1]Yi F, et al. Discovery of Novel Small-Molecule Inhibitors of LIM Domain Kinase for Inhibiting HIV-1. J Virol. 2017 Jun 9;91(13). pii: e02418-16.

[2]Paula Lunardi,et al. Effects of Hippocampal LIMK Inhibition on Memory Acquisition, Consolidation, Retrieval, Reconsolidation, and Extinction. Mol Neurobiol.2018 Feb;55(2):958-967.

[3]Yanghong Meng,et al. Regulation of spine morphology and synaptic function by LIMK and the actin cytoskeleton. Rev Neurosci. 2003;14(3):233-40.

[4]Lei Tian,et al. A study of the expression and interaction of Destrin, cofilin, and LIMK in Debakey I type thoracic aortic dissection tissue. Scand J Clin Lab Invest. 2010 Nov;70(7):523-8.