Background
Serine/arginine-rich protein-specific kinases (SRPKs) 1 and 2 phosphorylate and regulate serine/arginine-rich (SR) proteins that bind and regulate mRNA splicing, playing an important role in post-transcriptional regulation (1). The small-molecule SRPIN340 is an SRPK inhibitor that is highly selective for SRPK1 (Ki = 0.89 mM) and SRPK2. SRPK dysregulation can alter SR protein activity and promote expression of splicing isoforms, leading to increased viral infection or tumorigenic processes. Inhibition of SRPK1 and SRPK2 by SRPIN340 reduces SRp75 protein phosphorylation, leading to suppressed Sindbis virus propagation and reduced HIV production (2). Dose-dependent suppression of hepatitis C virus replication by the inhibitor SRPIN340 has been seen in vitro (1). SRPIN340 treatment of leukemia cells triggered early and late events of apoptosis, and reduced myeloid and lymphoid leukemia cell viability (3). Suppression of VEGF by SRPIN340 inhibited choroidal neovascularization formation in a mouse model, suggesting a possible role for SRPIN340 in treating neovascular age-related macular degeneration (4).
Molecular Formula
C18H18F3N3O
Molecular Weight
349.4 g/mol
Purity
>98%
CAS
218156-96-8
Solubility
Soluble in DMSO at 40 mg/mL or ethanol at 25 mg/mL.
Storage
Directions for Use
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
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