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

Ficha de datos de seguridad (MSDS o SDS), certificado de análisis y de calidad (CoA y CoQ), expedientes, folletos y otros documentos disponibles.

Sinónimos: N-(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

504293
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Descripción

Replacement Information

Tabla espec. clave

CAS #Empirical Formula
218156-96-8C₁₈H₁₈F₃N₃O

Products

Número de referenciaEmbalaje Cant./Env.
5042930001 Frasco de vidrio 10 mg
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 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
Número de referencia GTIN
5042930001 04055977263909

Documentation

SRPK Inhibitor, SRPIN340 - CAS 218156-96-8 - Calbiochem Ficha datos de seguridad (MSDS)

Título

Ficha técnica de seguridad del material (MSDS) 

Referencias bibliográficas

Visión general referencias
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.
Ficha técnica

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 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.