LIMKi 3 (Synonyms: LIM Kinase Inhibitor I, LIMKi 3) |
| Catalog No.GC15511 |
LIMKi 3 (LIMKi 3) is a potent LIMK inhibitor with IC50s of 7 nM and 8 nM for LIMK1 and LIMK2, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Synonyms | LIM Kinase Inhibitor I, LIMKi 3 | ||
| Chemical Name | 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 | ||
| Formula | C17H14Cl2F2N4OS | M.Wt | 431.29 |
| Solubility | DMF: 15 mg/ml,DMSO: 25 mg/ml,DMSO:PBS (pH 7.2)(1:5): 0.2 mg/ml,Ethanol: 1 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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