85-2076-96　SRPK Inhibitor, SRPIN340 (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) 10mg　CAS No:281856-96-8　217809

特徴

• A cell-permeable isonicotinamide that acts as an ATP-competitive SRPK1-selective inhibitor (IC50 = 0.14 and 1.8uM, 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 (1h 10uM SRPIN340 prior to 12h IGF-1 stimulation of PCIPs) and in a murine hypoxia-induced retinal neovascularization model in vivo (10pmol/uL/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 = 60uM in Vero cultures) and HCV-JFH1 replication (1 & 10uM SRPIN340 in Huh7.5.1 cultures). Exhibits no toxicity toward rats (2g/kg p.o. for 2 wks), CHO (5mg/ml for 24h), or Huh7 (30uM for 48h).
• Synonyms: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
• Formula:C18H18F3N3O
• Solubility:DMSO
• Molar Mass:349.4
• Storage and Stability:Store at 4°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.