SRPIN340, a serine-arginine-rich protein kinase (SRPK) inhibitor, has a Ki of 0.89 μM for SRPK1 and inhibits SRPK2. It does not significantly affect other SRPKs like Clk1 and Clk4. SRPIN340 leads to the degradation of SRp75, essential for HIV expression, and inhibits the propagation of Sindbis virus and severe acute respiratory syndrome virus with an IC50 of 60 μM [1]. SRPIN340 displays inhibitory effects on leukemia cell lines such as AML HL60, ALL-T Molt4, and Jurkat, with IC50 values of 44.7 μM, 92.2 μM, and 82.3 μM, respectively [2].
体外研究
SRPIN340, a serine-arginine-rich protein kinase (SRPK) inhibitor, has a Ki of 0.89 μM for SRPK1 and inhibits SRPK2. It does not significantly affect other SRPKs like Clk1 and Clk4. SRPIN340 leads to the degradation of SRp75, essential for HIV expression, and inhibits the propagation of Sindbis virus and severe acute respiratory syndrome virus with an IC50 of 60 μM [1].
SRPIN340 displays inhibitory effects on leukemia cell lines such as AML HL60, ALL-T Molt4, and Jurkat, with IC50 values of 44.7 μM, 92.2 μM, and 82.3 μM, respectively [2].
SRPIN340 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HEK293 cells
10, 20, 50 µM
12 hours
SRPIN340 promotes degradation of SRp75
Proc Natl Acad Sci U S A. 2006 Jul 25;103(30):11329-33.
HeLa cells
10 µM
16 hours
SRPIN340 showed minimal effect on SR protein phosphorylation at 10 μM concentration
Cell Chem Biol. 2018 Apr 19;25(4):460-470.e6.
Vero cells
40 µM
20 hours
SRPIN340 inhibits cytopathic effect of Sindbis virus
Proc Natl Acad Sci U S A. 2006 Jul 25;103(30):11329-33.
Invest Ophthalmol Vis Sci. 2013 Aug 27;54(8):5797-806.
ARPE-19 cells
10 µM
24 hours
SRPIN340 significantly increased the expression of VEGF xxxb protein isoforms relative to total VEGF in ARPE-19 cells
Invest Ophthalmol Vis Sci. 2013 Aug 27;54(8):5797-806.
PBLs from ENKTL patients
12.5 µM
24 hours
SRPK1 inhibitors decreased cell activity and increased apoptosis
BMC Cancer. 2022 Oct 27;22(1):1100.
YT cells
12.5 µM
24 hours
SRPK1 inhibition significantly reduced YT cell viability and induced apoptosis
BMC Cancer. 2022 Oct 27;22(1):1100.
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.
Br J Cancer. 2014 Jul 29;111(3):477-85.
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.
Br J Cancer. 2014 Jul 29;111(3):477-85.
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.
Br J Cancer. 2014 Jul 29;111(3):477-85.
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.
Br J Cancer. 2014 Jul 29;111(3):477-85.
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.
Mol Oncol. 2024 Oct;18(10):2510-2523.
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.
Mol Oncol. 2024 Oct;18(10):2510-2523.
T24 cells
5–80 µM
48 hours
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.
Cells. 2021 Mar 30;10(4):759.
HeLa cells
5–80 µM
48 hours
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.
Cells. 2021 Mar 30;10(4):759.
MDA PCa 2b
25 µM
48 hours
Inhibition of SRSF2 activity enhances sensitivity of PI3Kδ inhibitors to PI3Kδ-S-expressing cells
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.
Front Endocrinol (Lausanne). 2023 Aug 21;14:1190479.
Huh7 cells
30 µM
48 hours
SRPIN340 significantly suppressed HCV core antigen secretion and intracellular core protein expression in HCV-JFH1-infected Huh7 cells.
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).
Br J Cancer. 2014 Jul 29;111(3):477-85.
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
Invest Ophthalmol Vis Sci. 2013 Aug 27;54(8):5797-806.
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