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LIMKi 3

现货
Catalog No.
B7707
LIMK1和LIMK2抑制剂
组合的产品项目
规格价格库存 数量
10mg
¥ 2,640.00
Ship with 10-15 days

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Background

LIMKi 3 is a novel small molecule inhibitor of LIMK1 and LIMK2 with IC50 values of 7 and 8 nM, respectively [1].

LIM kinase (LIMK) includes LIMK1 and LIMK2, which regulate the actin polymerization mediated by the Rho family (Rho, Rac, and Cdc42) and the actin cytoskeleton by phosphorylating and inactivating the cofilin family of actin-depolymerizing factors. The functions of LIMK contribute to its irreplaceable effects in cell movement, division and structure formation[1] [3].

In vitro: In human breast cancer cells MDA-MB-231, treatment with LIMKi 3 (0~10 μM) resulted in the inhibition of LIMK activity and cofilin phosphorylation in a dose-dependent manner, induced a reduction in F-actin signal intensity and serum-stimulated SRF activity. LIMK inhibition also reduced matrigel invasion in three-dimensional invasion assays, but had no effect on microtubule number or organization and wound healing. Although motility was unaffected, LIMK inhibition by LIMKi 3 impaired matrix protein degradation[2].

References:
[1] Ross-Macdonald P, De S H, Guo Q, et al.  Identification of a nonkinase target mediating cytotoxicity of novel kinase inhibitors.[J]. Molecular Cancer Therapeutics, 2008, 7(11):3490-3498.
[2] Scott R W, Hooper S, Crighton D, et al.  LIM kinases are required for invasive path generation by tumor and tumor-associated stromal cells.[J]. Journal of Cell Biology, 2010, 191(1):169-85.
[3] Jia R X, Duan X, Song S J, et al.  LIMK1/2 inhibitor LIMKi 3 suppresses porcine oocyte maturation[J]. Peerj, 2016, 2016(10).

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt431.29
Cas No.1338247-35-0
FormulaC17H14Cl2F2N4OS
SolubilitySoluble in DMSO
Chemical NameN-(5-(1-(2,6-dichlorophenyl)-3-(difluoromethyl)-1H-pyrazol-5-yl)thiazol-2-yl)isobutyramide
SDFDownload SDF
Canonical SMILESClC1=[C@@](C(Cl)=CC=C1)[N@@]2N=C(C(F)F)C=C2C3=CN=C(NC(C(C)C)=O)S3
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

人乳腺癌细胞MDA-MB-231

溶解方法

在DMSO中的溶解度为> 10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应时间

24 h,0~10 μM

应用

MDA-MB-231细胞经LIMKi 3(0~10 μM)处理后, LIMK的活性受到抑制,LIMKi 3剂量依赖性地抑制丝切蛋白的磷酸化,减少肌动蛋白的信号强度和血清刺激的SRF活性。LIMKi 3对微管数量和组织没有影响。在3D基质胶侵袭实验中,3 μM LIMKi 3显著抑制基质胶的侵袭,0.1~3 μM LIMKi 3对伤口愈合没有影响,10 μM LIMKi 3显著抑制细胞的明胶降解面积。LIMKi 3虽然不影响细胞的运动,但是能减弱基质蛋白的降解。

References:

[1] Scott R W, Hooper S, Crighton D, et al. LIM kinases are required for invasive path generation by tumor and tumor-associated stromal cells.[J]. Journal of Cell Biology, 2010, 191(1):169-85.

质量控制

质量控制和MSDS

批次:

化学结构

LIMKi 3