SRPIN340

製品コードS7270 バッチS727001

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₈H₁₈F₃N₃O
	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.

溶剤液（一定の濃度）を調合する

生物活性

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

プロトコル(参考用のみ)

キナーゼアッセイ	In Vitro Kinase Assay and Kinetic Analysis
キナーゼアッセイ	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.

参考

カスタマーフィードバック

: 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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

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