R112

製品コードS6519 バッチS651901

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₁₆H₁₃FN₄O₂
	分子量	312.30	CAS No.	575474-82-7
Solubility (25°C)*	体外	DMSO	62 mg/mL (198.52 mM)
		Water	Insoluble
		Ethanol	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	R112 is an ATP-competitive spleen tyrosine kinase (Syk) inhibitor with Ki value of 96 nM.
in vitro	R112 inhibits degranulation induced by anti-IgE cross-linking in mast cells (tryptase release, effective concentration for 50% inhibition [EC50] = 353 nmol/L) or basophils (histamine release, EC50 = 280 nmol/L), and by allergen (dust mite) in basophils (histamine release, EC50 = 490 nmol/L). R112 also blocks leukotriene C4 production and all proinflammatory cytokines tested. Its onset of action is immediate, and the inhibition is reversible. R112 is able to completely inhibit all three IgE-induced mast cell functions: degranulation, lipid mediator production, and cytokine production. R112 does not inhibit phosphorylation of the Lyn target Syk (Y352), but inhibits the phosphorylation of the Syk target LAT (Y191), indicating that Syk kinase is the primary target of R112. Most phosphorylation events downstream of Syk are inhibited with similar potency by R112. In vitro kinase assays do not always correlate with the corresponding activity inside cells. R112 inhibits the Lyn kinase in vitro assay with an IC50 of 0.3 μmol/L; however, as mentioned previously, in CHMCs (Cultured human mast cells), R112 does not inhibit the phosphorylation of Syk (Y352), and therefore most likely does not inhibit Lyn activity^[1].

製品説明

R112 is an ATP-competitive spleen tyrosine kinase (Syk) inhibitor with Ki value of 96 nM.

in vitro

R112 inhibits degranulation induced by anti-IgE cross-linking in mast cells (tryptase release, effective concentration for 50% inhibition [EC50] = 353 nmol/L) or basophils (histamine release, EC50 = 280 nmol/L), and by allergen (dust mite) in basophils (histamine release, EC50 = 490 nmol/L). R112 also blocks leukotriene C4 production and all proinflammatory cytokines tested. Its onset of action is immediate, and the inhibition is reversible. R112 is able to completely inhibit all three IgE-induced mast cell functions: degranulation, lipid mediator production, and cytokine production. R112 does not inhibit phosphorylation of the Lyn target Syk (Y352), but inhibits the phosphorylation of the Syk target LAT (Y191), indicating that Syk kinase is the primary target of R112. Most phosphorylation events downstream of Syk are inhibited with similar potency by R112. In vitro kinase assays do not always correlate with the corresponding activity inside cells. R112 inhibits the Lyn kinase in vitro assay with an IC50 of 0.3 μmol/L; however, as mentioned previously, in CHMCs (Cultured human mast cells), R112 does not inhibit the phosphorylation of Syk (Y352), and therefore most likely does not inhibit Lyn activity^[1].

プロトコル(参考用のみ)

参考

[1] Rossi AB, et al. J Allergy Clin Immunol. 2006, 118(3):749-55.

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。