CasNo.218156-96-8,SRPIN 340 ,,(218156-96-8) Suppliers

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Keywords

SRPIN 340 , SRPIN 340;SRPIN340;SRPIN-340;SRPK inhibitor;N-(2-(piperidin-1-yl)-5-(trifluoroMethyl)phenyl)isonicotinaMide;N-[2-(1-Piperidinyl)-5-(trifluoromethyl)phenyl]-4-pyridinecarboxamide;SRPK Inhibitor(SRPIN34 218156-96-8

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Appearance:off white powder
Application:CAS：218156-96-8； Small molecule inhibitors
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ProductionCapacity:1000|Gram|Week
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Details:

SRPIN340 is a serine/arginine-rich protein kinase (SRPK)-specific inhibitor with an IC50 value of 0.89 uM (SRPK1); no significant inhibitory activity against more than 140 other kinases.
IC50 Value: 0.89 uM (SRPK1) [1]
Target: SRPK
in vitro: SRPIN340 potently inhibits SRPK1 kinase activity, with a Kivalue of 0.89 μM. SRPIN340 inhibits SR phosphorylation by SRPK in Flp-In293 cells and promotes degradation of SRp75 in a dose-dependent manner (Fig. 4). Thus, because retention of SRp75 is necessary for HIV expression, SRPIN340 emerges as a potential inhibitor of HIV production. SRPIN340 (40 μM) rescues Vero cells from the cytopathic effect of Sindbis virus. The SRPIN340 IC50 for Sindbis virus propagation was 60 μM [1]. SRPIN340, suppressed in a dose-dependent fashion expression of a hepatitis C virus (HCV) subgenomic replicon and replication of the HCV-JFH1 clone in vitro. The inhibitory effects were not associated with antiproliferative or nonspecific cytotoxic effects on the host cells. Overexpression of SRPK1 or SRPK2 resulted in augmentation of HCV replication, while small interfering RNA (siRNA) knockdown of the SRPKs suppressed HCV replication significantly [2]. SRPIN340 inhibited CNV formation in a dose-dependent manner. Compared with the vehicle, SRPIN340 significantly decreased the protein levels of VEGF, MCP-1, ICAM-1, and consequently inhibited macrophage infiltration. Furthermore, SRPIN340 suppressed the gene expression levels of total Vegf and exon 8a-containing Vegf isoforms [3].
in vivo: No adverse effects were observed when SRPIN340 was orally administrated to rats, even at the highest SRPIN340 dose (2,000 mg/kg). In addition, no abnormalities in chromosomal structure and chromosome number were observed when SRPIN340 was administrated to CHO cells in the culture medium at the highest SRPIN340 dose (5 mg/ml) for 24 h [1].
Toxicity: The rudimentary toxicity data available for SRPIN340 is promising with respect to the potential for use of this compound as a therapeutic. No adverse effects were observed when SRPIN340 was orally administrated to rats, even at the highest SRPIN340 dose (2,000 mg/kg). In addition, no abnormalities in chromosomal structure and chromosome number were observed when SRPIN340 was administrated to CHO cells in the culture medium at the highest SRPIN340 dose (5 mg/ml) for 24 h [1].
Clinical trial: