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504293 SRPK Inhibitor, SRPIN340 - CAS 218156-96-8 - Calbiochem

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Synonyme: Serine-Arginine-Rich Protein Kinase Inhibitor, SR Protein Kinase Inhibitor, SR Protein Phosphorylation Inhibitor 340, (SRPIN)340, N-(2-Piperidin-1-yl-5-(trifluoromethyl)phenyl)isonicotinamide

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504293
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Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
218156-96-8C₁₈H₁₈F₃N₃O

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      Description
      OverviewA cell-permeable isonicotinamide that acts as an ATP-competitive SRPK1-selective inhibitor (IC50 = 0.14 and 1.8 µM, respectively, against mSRPK1 and mSRPK2) with much reduced activity against 143 other kinases. Shown to effectively counteract IGF-1-induced anti-angiogenic to pro-angiogenic VEGF isoforms switch both in cultures in vitro (1 h 10 µM SRPIN340 prior to 12 h IGF-1 stimulation of PCIPs) and in a murine hypoxia-induced retinal neovascularization model in vivo (10 pmol/µL/eye intraocular SRPIN340 injection) by inhibiting PKC/SRPK signaling-dependent, alternate splicing factor ASF- (SF2; splicing factor 2) mediated VEGF pro-mRNA PSS (proximal splice site) selection. Suppresses RNA virus Sindbis propagation (IC50 = 60 µM in Vero cultures) and HCV-JFH1 replication (1 & 10 µM SRPIN340 in Huh7.5.1 cultures). Exhibits no toxicity toward rats (2 g/kg p.o. for 2 wks), CHO (5 mg/mL for 24 h), or Huh7 (30 µM for 48 h).
      Catalogue Number504293
      Brand Family Calbiochem®
      SynonymsSerine-Arginine-Rich Protein Kinase Inhibitor, SR Protein Kinase Inhibitor, SR Protein Phosphorylation Inhibitor 340, (SRPIN)340, N-(2-Piperidin-1-yl-5-(trifluoromethyl)phenyl)isonicotinamide
      References
      ReferencesKarakama, Y., et al. 2010. Antimicrob. Agents Chemother. 54, 3179.
      Nowak, D.G., et al. 2010. J. Biol. Chem. 285, 5532.
      Fukuhara, T., et al. 2006. Proc. Natl. Acad. Sci. USA 103, 11329.
      Product Information
      CAS number218156-96-8
      FormLight beige powder
      Hill FormulaC₁₈H₁₈F₃N₃O
      Chemical formulaC₁₈H₁₈F₃N₃O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥99% by HPLC
      Physicochemical Information
      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
      Bestellnummer GTIN
      5042930001 04055977263909

      Documentation

      SRPK Inhibitor, SRPIN340 - CAS 218156-96-8 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Karakama, Y., et al. 2010. Antimicrob. Agents Chemother. 54, 3179.
      Nowak, D.G., et al. 2010. J. Biol. Chem. 285, 5532.
      Fukuhara, T., et al. 2006. Proc. Natl. Acad. Sci. USA 103, 11329.
      Datenblatt

      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.

      Revision17-July-2013 JSW
      SynonymsSerine-Arginine-Rich Protein Kinase Inhibitor, SR Protein Kinase Inhibitor, SR Protein Phosphorylation Inhibitor 340, (SRPIN)340, N-(2-Piperidin-1-yl-5-(trifluoromethyl)phenyl)isonicotinamide
      DescriptionAA cell-permeable isonicotinamide compound that acts as an ATP-competitive (Ki = 0.89 µM using mSRPK1), SRPK1-selective inhibitor (IC50 = 0.14 and 1.8 µM, respectively, against mSRPK1- or mSRPK2-catalyzed SF2 RS domain peptide phosphorylation) with much reduced or no activity against 143 other kinases, including Clk1 and Clk4, even at concentrations as high as 10 µM. Shown to effectively counteract IGF-1-induced anti-angiogenic to pro-angiogenic VEGF isoforms switch both in cultures in vitro (pro/anti VEGF mRNA ratio = 1.26- and 4.48-times of control ratio, respectively, in 12 h IGF-1 stimulated PCIPs with or without 1 h 10 µM SRPIN340 pretreatment) and in a murine hypoxia-induced retinal neovascularization model in vivo (Relative retinal VEGF mRNA content = 0.3 vs. 1.1, respectively, with or without 10 pmol/µL/eye intraocular SRPIN340 injection upon 48 h room air exposure of 6-day 75% O2-adopted P12 neonatal mice) by inhibiting PKC/SRPK signaling-dependent, alternate splicing factor ASF- (SF2; splicing factor 2) mediated VEGF pro-mRNA PSS (proximal splice site) selection. Suppresses RNA virus Sindbis propagation (IC50 = 60 µM as determined by virus titre in 4 d-infected Vero cultures) and HCV-JFH1 replication (% HCV core protein-positive Huh7.5.1 48 h post infection = 18.2, 5.9, and 3.0, respectively, with 0. 1. 10 µM SRPIN340; MOI = 0.1). Exhibits no mutagenic effects by Salmonella typhimurium AMES test, nor toxicity toward rats (2 g/kg p.o. for 2 wks), CHO (5 mg/mL for 24 h), or Huh7 (30 µM for 48 h).
      FormLight beige powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number218156-96-8
      Chemical formulaC₁₈H₁₈F₃N₃O
      Structure formulaStructure formula
      Purity≥99% 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
      ReferencesKarakama, Y., et al. 2010. Antimicrob. Agents Chemother. 54, 3179.
      Nowak, D.G., et al. 2010. J. Biol. Chem. 285, 5532.
      Fukuhara, T., et al. 2006. Proc. Natl. Acad. Sci. USA 103, 11329.