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435930 LIM Kinase Inhibitor I, LIMKi 3 - Calbiochem

Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1338247-35-0C₁₇H₁₄Cl₂F₂N₄OS

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435930-10MG
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      Description
      OverviewA cell-permeable pyrazolylthiazolo-isobutyramide compound that acts as a potent LIM kinase inhibitor (IC50 = 7 and 8 nM against LIMK1 and LIMK2, respectively) and effectively suppresses cellular cofilin phosphorylation (IC50 ~ 1 µM in A549 and MDA-MB-231 cultures) without affecting tubulin polymerization or inducing cytotoxicity (EC50 >10 µM in A549 proliferation & colony formation assays). Shown to effectively destabilize F-actin structure in MDA-MB-231 breast cancer cells (3 to 10 µM) with concomitant blockage of invasion (by 93% at 10 µM).
      Catalogue Number435930
      Brand Family Calbiochem®
      SynonymsN-(5-(1-(2,6-Dichlorophenyl)-3-(difluoromethyl)-1H-pyrazol-5-yl)thiazol-2-yl)isobutyramide
      References
      ReferencesScott, R.W., et al. 2010. J. Cell. Biol. 191, 169.
      Ross-Macdonald, P., et al. 2008. Mol. Cancer Ther. 7, 3490.
      Product Information
      CAS number1338247-35-0
      FormBeige powder
      Hill FormulaC₁₇H₁₄Cl₂F₂N₄OS
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationLIM Kinase Inhibitor I, LIMKi 3, CAS 1338247-35-0, is a cell-permeable, potent inhibitor of LIM kinase (IC50 = 7 & 8 nM against LIMK1 & LIMK2, respectively). Reduces MDA-MB-231 tumor cell invasion.
      Biological Information
      Primary TargetLIMK1 and LIMK2
      Primary Target IC<sub>50</sub>7 and 8 nM against LIMK1 and LIMK2, respectively
      Secondary targetAMPKA1, AMPKA2, DDR1, PAK3, DCAMKL2
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      435930-10MG 04055977210330

      Documentation

      LIM Kinase Inhibitor I, LIMKi 3 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      LIM Kinase Inhibitor I, LIMKi 3 - Calbiochem Certificates of Analysis

      TitleLot Number
      435930

      References

      Reference overview
      Scott, R.W., et al. 2010. J. Cell. Biol. 191, 169.
      Ross-Macdonald, P., et al. 2008. Mol. Cancer Ther. 7, 3490.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision22-November-2012 JSW
      SynonymsN-(5-(1-(2,6-Dichlorophenyl)-3-(difluoromethyl)-1H-pyrazol-5-yl)thiazol-2-yl)isobutyramide
      DescriptionA cell-permeable pyrazolylthiazolo-isobutyramide compound that acts as a potent LIM kinase inhibitor (IC50 = 7 and 8 nM against LIMK1 and LIMK2, respectively) and effectively suppresses cellular cofilin phosphorylation (IC50 ~ 1 µM in A549 and MDA-MB-231 cultures) without affecting tubulin polymerization or inducing cytotoxicity (EC50 >10 µM in A549 proliferation and colony formation assays). Shown to effectively destabilize F-actin structure in MDA-MB-231 breast cancer cells (3 to 10 µM) with concomitant blockage of invadopedia-mediated ECM degradation (13% and 10% of control, respectively, by 3 and 10 µM inhibitor) and invasion (45% and 7% of control invasion rate, respectively, by 3 and 10 µM inhibitor). Although reported to exhibit affinity toward AMPKα1 and AMPKα2 in T7 phage-based competition binding studies, inhibitory activity of LIMKi 3 against AMPKα1/2 is not yet directly demonstrated.
      FormBeige powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1338247-35-0
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesScott, R.W., et al. 2010. J. Cell. Biol. 191, 169.
      Ross-Macdonald, P., et al. 2008. Mol. Cancer Ther. 7, 3490.