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  6. 5042930001

MilliporeSigma™ Calbiochem™ SRPK Inhibitor, SRPIN340

Catalog No. 5042930001
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10mg

Description

A cell-permeable isonicotinamide that acts as an ATP-competitive SRPK1-selective inhibitor (IC50

A cell-permeable isonicotinamide that acts as an ATP-competitive SRPK1-selective inhibitor (IC50 = 0.14 and 1.8μM, 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 10μM 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 = 60μM in Vero cultures) and HCV-JFH1 replication (1 & 10μM SRPIN340 in Huh7.5.1 cultures). Exhibits no toxicity toward rats (2 g/kg p.o. for 2 wks), CHO (5mg/mL for 24 h), or Huh7 (30μM for 48 h).
TRUSTED_SUSTAINABILITY

Specifications

Color Light Beige
Description 99% by HPLC
Molecular Formula C18H18F3N3O
Formula Weight 349.4g/mol
Solubility DMSO
Content And Storage Protect from light
Form Powder
Quantity 10 mg
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