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538768 Lim Kinase Inhibitor II, SR-7826 - Calbiochem

A cell-permeable, highly potent and selective inhibitor of LIM kinase (IC₅₀ = 43 nM).

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 1-(2-Hydroxyethyl)-3-(4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)-1-phenylurea, LIMK Inhibitor, SR-7826

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538768
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      Description
      OverviewA cell permeable bis-aryl urea that acts as a highly potent and selective LIMK inhibitor (LIM kinase, IC50 = 43 nM for Limk1) with more than 400-fold selectivity against ROCK and JNK kinases. Only displays inhibitory effect on STK16 with ≥80% inhibition at 1 µM in addition to LIMK1 in a 61 kinase panel profiling. Inhibits cofilin phosphorylation in A7r5 (IC50 = 470 nM), PC-3 and CEM-SS T cells (IC50 < 1 µM), shown to inhibit cell invasion by 76% and cell migration by 74% in PC-3 cells at 1 µM. Exhibits desirable pharmacokinetic properties in vitro and in vivo with 36% bioavailability in rats (p.o. at 2mg/kg).

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number538768
      Brand Family Calbiochem®
      Synonyms1-(2-Hydroxyethyl)-3-(4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)-1-phenylurea, LIMK Inhibitor, SR-7826
      DescriptionLim Kinase Inhibitor II, SR-7826
      References
      ReferencesYin, Y., et al. 2015. J. Med. Chem. 58, 1846.
      Product Information
      FormOff-white solid
      Hill FormulaC₂₂H₂₁N₅O₂
      Chemical formulaC₂₂H₂₁N₅O₂
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetLIMK
      Purity≥98% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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 3 months at -20°C
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      5.38768.0001 04054839119668

      Documentation

      Lim Kinase Inhibitor II, SR-7826 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Yin, Y., et al. 2015. J. Med. Chem. 58, 1846.
      Fiche technique

      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.

      Revision23-September-2016 JSW
      Synonyms1-(2-Hydroxyethyl)-3-(4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)-1-phenylurea, LIMK Inhibitor, SR-7826
      DescriptionA cell permeable bis-aryl urea that acts as a highly potent and selective LIMK inhibitor (LIM kinase, IC50 = 43 nM for Limk1) with more than 400-fold selectivity against ROCK and JNK kinases. Only displays inhibitory effect on STK16 with ≥80% inhibition at 1 µM in addition to LIMK1 in a 61 kinase panel profiling. Inhibits cofilin phosphorylation in A7r5 (IC50 = 470 nM), PC-3 and CEM-SS T cells (IC50 < 1 µM), shown to inhibit cell invasion by 76% and cell migration by 74% in PC-3 cells at 1 µM. Exhibits desirable pharmacokinetic properties in vitro and in vivo with 36% bioavailability in rats (p.o. at 2mg/kg).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₂H₂₁N₅O₂
      Purity≥98% 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 3 months at -20°C
      Toxicity Standard Handling
      ReferencesYin, Y., et al. 2015. J. Med. Chem. 58, 1846.