Details
Stereochemistry | ACHIRAL |
Molecular Formula | C18H18F3N3O |
Molecular Weight | 349.3502 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
FC(F)(F)C1=CC=C(N2CCCCC2)C(NC(=O)C3=CC=NC=C3)=C1
InChI
InChIKey=DWFGGOFPIISJIT-UHFFFAOYSA-N
InChI=1S/C18H18F3N3O/c19-18(20,21)14-4-5-16(24-10-2-1-3-11-24)15(12-14)23-17(25)13-6-8-22-9-7-13/h4-9,12H,1-3,10-11H2,(H,23,25)
Molecular Formula | C18H18F3N3O |
Molecular Weight | 349.3502 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/16840555
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16840555
SRPIN340 was investigated as selective serine arginine protein kinase (SRPK) 1 inhibitor, it also could inhibit SRPK2 at higher concentrations, but did not significantly inhibit other SRPKs such as CLK1 and CLK4, or other classes of SR kinases. It was shown, that SRPIN340 targeted host proteins, and might be effective against multiple hepatitis C virus (HCV) genotypes. Furthermore, the toxicity data available for SRPIN340 were promising and no adverse effects were observed when SRPIN340 was administered orally to rats. On the other hand, the fact that this inhibitor acted through cellular components still raises concerns regarding its safety in the case of human use. Future studies with SRPIN340, its derivatives, and other chemicals that target SRPKs could be directed toward developing a new class of antiviral treatment regimens and drugs.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4375 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16840555 |
0.89 µM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
Utilization of host SR protein kinases and RNA-splicing machinery during viral replication. | 2006 Jul 25 |
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SRPK1 inhibition in vivo: modulation of VEGF splicing and potential treatment for multiple diseases. | 2012 Aug |
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SRPK1 inhibition modulates VEGF splicing to reduce pathological neovascularization in a rat model of retinopathy of prematurity. | 2013 Aug 27 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16840555
in rats (toxicity effect): No adverse effects were observed when SRPIN340 was orally administrated to rats, even at the highest SRPIN340 dose (2,000 mg/kg). 10 rats were observed for 2 weeks after SRPIN340 administration. All of the rats survived,
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16840555
SRPIN340 (40 μM) rescues Vero cells from the cytopathic effect of Sindbis virus. In a plaque assay with Vero cells, the SRPIN340 IC50 for Sindbis virus propagation was 60 μM. Preliminary studies indicate that SRPIN340 also suppresses propagation of severe acute respiratory syndrome virus. Thus, the kinase activities of SR protein kinase (SRPKs) appear to be required for propagation of a variety of RNA viruses. SRPIN340 in a dose-dependent manner (0, 10, 20 and 50 uM) inhibits SR phosphorylation by SRPK in Flp-In293 cells and promotes degradation of SRp75. Thus, because retention of SRp75 is necessary for HIV expression, SRPIN340 emerges as a potential inhibitor of HIV production
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 15:33:07 GMT 2023
by
admin
on
Sat Dec 16 15:33:07 GMT 2023
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Record UNII |
9QS4MR9N9D
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Record Status |
Validated (UNII)
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Record Version |
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