SRPIN340

Catalog No.S7270

SRPIN340 is a selective SRPK inhibitor with Ki of 0.89 μM for SRPK1, showing no significant inhibitory activity against more than 140 other kinases..

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SRPIN340 Chemical Structure

SRPIN340 Chemical Structure
Molecular Weight: 349.35

Validation & Quality Control

Quality Control & MSDS

Product Information

Product Description

Biological Activity

Description SRPIN340 is a selective SRPK inhibitor with Ki of 0.89 μM for SRPK1, showing no significant inhibitory activity against more than 140 other kinases..
Targets SRPK1 [1]
IC50 0.89 μM(Ki)
In vitro 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. [1] SRPIN340 suppresses in a dose-dependent fashion expression of a HCV subgenomic replicon and replication of the HCV-JFH1 clone in vitro. [2]
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. [3]
Features The only specific SRPK1 and SRPK2 inhibitor. Potential use in congenital diseases and viral diseases including HIV, HCV and HBV.

Protocol(Only for Reference)

Kinase Assay: [1]

In Vitro Kinase Assay and Kinetic Analysis Kinase activity of Clks and SRPKs is assayed in a reaction mixture, containing 200 mM Tris-HCl (pH 7.5), 12.5 mM MgCl2, 8 mM dithiothreitol, 4 mM EGTA, 1–20 μM ATP, 1 μCi of [γ-32P]ATP, 1 μg of synthetic peptide of SF2/ASF RS domain (NH2-RSPSYGRSRSRSRSRSRSRSRSNSRSRSY-OH), and 0.1–1 μg of purified kinases in a final volume of 40 μl. cAMP-dependent protein kinase activity was assayed in a reaction mixture containing 80 mM Tris-HCl (pH 7.5), 12.5 mM MgCl2, 8 mM dithiothreitol, 4 mM EGTA, 10 μM ATP, 1 μCi of [γ-32P]ATP, 5 μg of histone H1 (Sigma), and 1 μg of catalytic subunit of rat cAMP-dependent protein kinase purified. Protein kinase C activity is assayed in a reaction mixture containing 200 mM Tris-HCl (pH 7.5), 12.5 mM MgCl2, 1 mM CaCl2, 80 μg/ml phosphatidylserine, 8 μg/ml diolein, 10 μM ATP, 1 μCi of [γ-32P]ATP, 5 μg of histone H1, and 2 μl of partially purified rat protein kinase C. The final concentration of Me2SO is adjusted to 1% regardless of inhibitor concentration. The reaction mixture is incubated at 30 or 25 °C for mammalian or Xenopus recombinant proteins, respectively, for 10 min, and a half-portion is spotted on P81 phosphocellulose membrane (Whatman). The kinase assay conditions, including the incubation period and concentration of kinases and substrates, are optimized to maintain the linearity during incubation. The membrane is washed with 5% phosphoric acid solution (SF2/ASF RS domain) or 5% trichloroacetic solution (histone H1) at least over 15 min. The radioactivity is measured using a liquid scintillation counter. The net radioactivity is deduced by subtracting the background count from the reaction mixture without kinase, and the data are expressed as the percentage to the control sample containing the solvent.

Animal Study: [3]

Animal Models A mouse model with choroidal neovascularization (CNV)
Formulation DMSO
Dosages ~20 pmol
Administration i.v.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Fukuhara T, et al. Proc Natl Acad Sci U S A. 2006, 103(30), 11329-11333.

[2] Karakama Y, et al. Antimicrob Agents Chemother. 2010, 54(8), 3179-3186.

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Chemical Information

Download SRPIN340 SDF
Molecular Weight (MW) 349.35
Formula

C18H18F3N3O

CAS No. 218156-96-8
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 70 mg/mL (200.37 mM)
Ethanol 70 mg/mL (200.37 mM)
Water <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 8 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 4-Pyridinecarboxamide, N-[2-(1-piperidinyl)-5-(trifluoromethyl)phenyl]-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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