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Chemical Structure| 218156-96-8 Chemical Structure| 218156-96-8

Structure of SRPIN340
CAS No.: 218156-96-8

Chemical Structure| 218156-96-8

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SRPIN340 is an inhibitor of serine/arginine-rich protein kinase SRPK1 with IC50 of 0.89 μM.

Synonyms: SRPK inhibitor

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Product Details of SRPIN340

CAS No. :218156-96-8
Formula : C18H18F3N3O
M.W : 349.35
SMILES Code : O=C(NC1=CC(C(F)(F)F)=CC=C1N2CCCCC2)C3=CC=NC=C3
Synonyms :
SRPK inhibitor
MDL No. :MFCD00116244
InChI Key :DWFGGOFPIISJIT-UHFFFAOYSA-N
Pubchem ID :2797577

Safety of SRPIN340

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of SRPIN340

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK293 cells 10, 20, 50 μM 12 hours SRPIN340 promotes degradation of SRp75 PMC1544086
Vero cells 40 μM 20 hours SRPIN340 inhibits cytopathic effect of Sindbis virus PMC1544086
HeLa cells 10 μM 16 hours SRPIN340 showed minimal effect on SR protein phosphorylation at 10 μM concentration PMC5973797
Primary RPE cells 10μM 24 hours SRPIN340 significantly reduced pro-angiogenic VEGF expression PMC6485497
ARPE-19 cells 10μM 24 hours SRPIN340 significantly increased the expression of VEGF xxxb protein isoforms relative to total VEGF in ARPE-19 cells PMC6485497
PBLs from ENKTL patients 12.5 μM 24 hours SRPK1 inhibitors decreased cell activity and increased apoptosis PMC9609466
YT cells 12.5 μM 24 hours SRPK1 inhibition significantly reduced YT cell viability and induced apoptosis PMC9609466
92.1 1-10 μM 24-48 hours SRPIN340 reduced VEGF165 mRNA in a dose-dependent manner in all four cell lines tested. Furthermore, total VEGF protein was similarly reduced by SRPIN340 reaching significance at 10 μM in A375, Omm2.5 and 92.1 cells. PMC4119992
Mel270 1-10 μM 24-48 hours SRPIN340 reduced VEGF165 mRNA in a dose-dependent manner in all four cell lines tested. Furthermore, total VEGF protein was similarly reduced by SRPIN340 reaching significance at 10 μM in A375, Omm2.5 and 92.1 cells. PMC4119992
Omm2.5 1-10 μM 24-48 hours SRPIN340 reduced VEGF165 mRNA in a dose-dependent manner in all four cell lines tested. Furthermore, total VEGF protein was similarly reduced by SRPIN340 reaching significance at 10 μM in A375, Omm2.5 and 92.1 cells. PMC4119992
A375 1-10 μM 24-48 hours SRPIN340 reduced VEGF165 mRNA in a dose-dependent manner in all four cell lines tested. Furthermore, total VEGF protein was similarly reduced by SRPIN340 reaching significance at 10 μM in A375, Omm2.5 and 92.1 cells. PMC4119992
LNCaP-MYC prostate cancer cells 20 μM 4 days To evaluate the anti-proliferative effect of SRPIN340 on MYC-overexpressing cells, results showed SRPIN340 significantly inhibited cell proliferation. PMC11459032
22RV1 prostate cancer cells 20 μM 4 hours To assess the effect of SRPIN340 on nascent transcription, results showed SRPIN340 significantly upregulated transcription of long genes. PMC11459032
T24 cells 5–80 µM 48 h SRPIN340 significantly prevented the nuclear translocation of SRPK1 and SRPK2 in 5-FU and cisplatin-treated T24 cells, thus diminishing the cytotoxic effects of the drug. PMC8065462
HeLa cells 5–80 µM 48 h SRPIN340 significantly prevented the nuclear translocation of SRPK1 and SRPK2 in 5-FU and cisplatin-treated HeLa cells, thus diminishing the cytotoxic effects of the drug. PMC8065462
MDA PCa 2b 25 µM 48 hours Inhibition of SRSF2 activity enhances sensitivity of PI3Kδ inhibitors to PI3Kδ-S-expressing cells PMC9954641
Prostate cancer cells (22Rv1, LNCaP, MDA PCa 2b, HT-29, A549, MCF-7) 25 µM 48 hours To evaluate the inhibitory effect of SRPIN340 on the PIK3CD-S splice variant and its impact on the AKT/mTOR signaling pathway. Results showed that SRPIN340 treatment significantly reduced PIK3CD-S expression and inhibited the AKT/mTOR signaling pathway. PMC10475954
Huh7 cells 30 µM 48 hours SRPIN340 significantly suppressed HCV core antigen secretion and intracellular core protein expression in HCV-JFH1-infected Huh7 cells. PMC2916360
Huh7/Rep-Feo-2a cells 15.8 µM (EC50) 48 hours SRPIN340 suppressed HCV 2a subgenomic replicon expression in a dose-dependent manner with an EC50 of 15.8 µM. PMC2916360
Huh7/Rep-Feo-1b cells 4.7 µM (EC50) 48 hours SRPIN340 suppressed HCV 1b subgenomic replicon expression in a dose-dependent manner with an EC50 of 4.7 µM. PMC2916360

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Subcutaneous xenograft model Subcutaneous injection 2 mg Daily for 27 days SRPIN340 significantly reduced tumour growth and decreased total VEGF expression in tumours, but did not affect anti-angiogenic VEGF xxxb isoforms. Additionally, SRPIN340 significantly reduced microvascular density (MVD). PMC4119992
Sprague Dawley rats 50/10 Oxygen Induced Retinopathy model Intraocular injection 25 ng Single injection SRPIN340 significantly reduced PRNV and decreased pro-angiogenic VEGF expression PMC6485497

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.86mL

0.57mL

0.29mL

14.31mL

2.86mL

1.43mL

28.62mL

5.72mL

2.86mL

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