435930 LIM Kinase Inhibitor I, LIMKi 3 - Calbiochem

435930
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₇H₁₄Cl₂F₂N₄OS 1338247-35-0

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      435930-10MG
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          Glass bottle 10 mg
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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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          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 +2°C to +8°C
          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.
          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.