504293 SRPK Inhibitor, SRPIN340 - CAS 281856-96-8 - Calbiochem

504293
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₈H₁₈F₃N₃O 281856-96-8

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.04293.0001
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          Glass bottle 10 mg
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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®
          SynonymsN-(2-Piperidin-1-yl-5-(trifluoromethyl)phenyl)isonicotinamide, Serine-Arginine-Rich Protein Kinase Inhibitor, SR Protein Kinase Inhibitor, SR Protein Phosphorylation Inhibitor 340, (SRPIN)340
          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 number281856-96-8
          FormLight beige powder
          Hill FormulaC₁₈H₁₈F₃N₃O
          Chemical formulaC₁₈H₁₈F₃N₃O
          Structure formula ImageStructure formula Image
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          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.
          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.

          Revision17-July-2013 JSW
          SynonymsN-(2-Piperidin-1-yl-5-(trifluoromethyl)phenyl)isonicotinamide, Serine-Arginine-Rich Protein Kinase Inhibitor, SR Protein Kinase Inhibitor, SR Protein Phosphorylation Inhibitor 340, (SRPIN)340
          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 number281856-96-8
          Chemical formulaC₁₈H₁₈F₃N₃O
          Structure formulaStructure formula
          Purity≥99% 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
          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.