LIMKi 3
(Synonyms: LIMKi 3) 目录号 : GC15511
An inhibitor of LIMK1 and LIMK2
Cas No.:1338247-35-0
Sample solution is provided at 25 µL, 10mM.
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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).
| Cell experiment [1]: | |
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Cell lines |
Human breast cancer cells MDA-MB-231 |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
24 h, 0~10 µM |
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Applications |
In MDA-MB-231 cells, LIMKi 3 potently inhibited LIMK activity, the treatment with LIMKi 3 (0~10 µM) resulted in a dose-dependent inhibition of cofilin phosphorylation, induced a reduction in F-actin signal intensity and serum-stimulated SRF activity. LIMKi 3 had no effect on microtubule number or organization. 3 µM LIMKi 3 significantly inhibited matrigel invasion in the 3D matrigel invasion assay, 0.1~3 µM LIMKi 3 had no effect on wound healing. 10 µM LIMKi 3 significantly reduced the area of gelatin degradation per cell. Although motility was unaffected, LIMK inhibition by LIMKi 3 impaired matrix protein degradation. |
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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. | |
| Cas No. | 1338247-35-0 | SDF | |
| 别名 | LIMKi 3 | ||
| 化学名 | N-(5-(1-(2,6-dichlorophenyl)-3-(difluoromethyl)-1H-pyrazol-5-yl)thiazol-2-yl)isobutyramide | ||
| Canonical SMILES | ClC1=[C@@](C(Cl)=CC=C1)[N@@]2N=C(C(F)F)C=C2C3=CN=C(NC(C(C)C)=O)S3 | ||
| 分子式 | C17H14Cl2F2N4OS | 分子量 | 431.29 |
| 溶解度 | DMF: 15 mg/ml,DMSO: 25 mg/ml,DMSO:PBS (pH 7.2)(1:5): 0.2 mg/ml,Ethanol: 1 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3186 mL | 11.5931 mL | 23.1863 mL |
| 5 mM | 0.4637 mL | 2.3186 mL | 4.6373 mL |
| 10 mM | 0.2319 mL | 1.1593 mL | 2.3186 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet