product name SRPIN340
Description: SRPIN340 is a potent and selective SRPK inhibitor with Ki of 0.89 μM for SRPK1, it exhibited no significant inhibitory activity against more than 140 other kinases. SRPIN340 has been revealed to inhibit replication of HIV-1 and other viruses that require SR protein-dependent RNA processing for the propagation in HIV-1 transfected or infected Flp-In293 cell lines. In addition, SRPIN340 has been reported to significantly inhibit SRPK1 and SRPK2 kinase activity but not potently inhibit other SRPKs, such as Clk1 and Clk4 with a Ki value of 0.89μM for SRPK1.
References: Proc Natl Acad Sci U S A. 2006 Jul 25;103(30):11329-33; Antimicrob Agents Chemother. 2010 Aug;54(8):3179-86; Mol Vis. 2013;19:536-43.
349.35
Formula
C18H18F3N3O
CAS No.
218156-96-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 70 mg/mL (200.4 mM)
Water: <1 mg/mL
Ethanol: 70 mg/mL (200.4 mM)
Solubility (In vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 8 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: SRPIN340 inhibits SR phosphorylation by SRPK in Flp-In293 cells and promotes degradation of SRp75 in a dose-dependent manner, which subsequently inhibits HIV production. SRPIN340 dose (5 mg/mL) produces no abnormalities in chromosomal structure and chromosome number of CHO cells. SRPIN340 suppresses in a dose-dependent fashion expression of a HCV subgenomic replicon and replication of the HCV-JFH1 clone in vitro. Kinase Assay: Cell Assay: SRPIN340 has been revealed to inhibit replication of HIV-1 and other viruses that require SR protein-dependent RNA processing for the propagation in HIV-1 transfected or infected Flp-In293 cell lines. In addition, SRPIN340 has been reported to significantly inhibit SRPK1 and SRPK2 kinase activity but not potently inhibit other SRPKs, such as Clk1 and Clk4 with a Ki value of 0.89μM for SRPK1. Besides, SRPIN340 has been exhibited to dose-dependently promote degradation of SRp75 which is necessary for HIV expression. Moreover, SRPIN340 has shown the inhibition of propagation of Sindbis virus with an IC50 of 60μM and the protection against the cytopathic effect of Sindbis virus. |
|---|---|
| In Vivo | SRPIN340 inhibits CNV formation in a dose-dependent manner in vivo. SRPIN340 significantly decreases the protein levels of VEGF, MCP-1, ICAM-1, and consequently inhibits macrophage infiltration. |
| Animal model | A mouse model with choroidal neovascularization (CNV) |
| Formulation & Dosage | Dissolved in DMSO; ~20 pmol; i.v. |
| References | Proc Natl Acad Sci U S A. 2006 Jul 25;103(30):11329-33; Antimicrob Agents Chemother. 2010 Aug;54(8):3179-86; Mol Vis. 2013;19:536-43. |
