受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C18H18F3N3O |
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分子量 | 349.35 | CAS No. | 218156-96-8 | |
Solubility (25°C)* | 体外 | DMSO | 70 mg/mL (200.37 mM) | |
Ethanol | 70 mg/mL (200.37 mM) | |||
Water | Insoluble | |||
* <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. |
製品説明 | 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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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] |
特徴 | The only specific SRPK1 and SRPK2 inhibitor. Potential use in congenital diseases and viral diseases including HIV, HCV and HBV. |
キナーゼアッセイ | In Vitro Kinase Assay and Kinetic Analysis | |
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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. | ||
動物実験 | 動物モデル | A mouse model with choroidal neovascularization (CNV) |
投薬量 | ~20 pmol | |
投与方法 | i.v. |
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Data from [Data independently produced by , , Cell, 2017, 171(7):1545-1558]
Data from [Data independently produced by , , Cell, 2017, 171(7):1545-1558.e18]
The Spliceosome: A New Therapeutic Target in Chronic Myeloid Leukaemia [ Cancers (Basel), 2022, 14(19)4695] | PubMed: 36230624 |
Actionable Cytopathogenic Host Responses of Human Alveolar Type 2 Cells to SARS-CoV-2 [ Mol Cell, 2020, 80(6):1104-1122.e9] | PubMed: 33259812 |
Post-transcriptional Regulation of De Novo Lipogenesis by mTORC1-S6K1-SRPK2 Signaling. [Lee G, et al. Cell, 2017, 171(7):1545-1558] | PubMed: 29153836 |
hnRNP L controls HPV16 RNA polyadenylation and splicing in an Akt kinase-dependent manner. [ Nucleic Acids Res, 2017, 45(16):9654-9678] | PubMed: 28934469 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。