CAY10526

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CAY10526

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

938069-71-7

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议
10mg	电议

产品介绍

CAY10526 是一种特异性微粒体 PGE2 合酶-1 (mPGES1) 抑制剂。 CAY10526 通过选择性调节 mPGES1 表达抑制 PGE2 的产生，但不影响 COX-2。 CAY10526 在黑色素瘤异种移植物中显着抑制肿瘤生长并增加细胞凋亡。 CAY10526 降低 BCL-2 和 BCL-XL（抗凋亡）蛋白水平并增加 BAX 和 BAK（促凋亡）以及切割的 caspase 3 水平。 CAY10526 在三种表达 mPGES1 的黑色素瘤细胞系中抑制细胞活力 (IC50<5 μM)。

Cas No.	938069-71-7
化学名	4-(benzo[b]thiophen-2-yl)-3-bromo-5-hydroxydihydrofuran-2(3H)-one
Canonical SMILES	O=C1OC(O)C(C2=CC(C=CC=C3)=C3S2)=C1Br
分子式	C₁₂H₇BrO₃S
分子量	311.1
溶解度	1mg/ml in ethanol; 30mg/ml in DMSO & DMF
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	Prostaglandin E2 (PGE2) is the major PG synthesized at sites of inflammation and plays an important role in different inflammatory diseases. It acts as a mediator of pain and inflammation and promotes bone destruction. The increased synthesis of PGE2 during inflammation can be accounted for by increased expression of both cyclooxygenase-2 (COX-2) and microsomal PGE synthase-1 (mPGES-1).[1],[2],[3] CAY10526 is an inhibitor of PGE2 production through the selective modulation of mPGES-1 expression. It dose-dependently inhibits PGE2 production in lipopolysaccharide-stimulated RAW 264.7 cells with an IC50 value of 1.8 μM without any effect on COX-2 expression.[4] Reference: [1]. Claveau, D., Sirinyan, M., Guay, J., et al. Microsomal prostaglandin E synthase-1 is a major terminal synthase that is selectively up-regulated during cyclooxygenase-2-dependent prostaglandin E2 production in the rat adjuvant-induced arthritis model. Journal of Immunology 170, 4738-4744 (2003). [2]. Guay, J., Bateman, K., Gordon, R., et al. Carrageenan-induced paw edema in rat elicits a predominant prostaglandin E2 (PGE2) response in the central nervous system associated with the induction of microsomal PGE2 synthase-1. The Journal of Biological Chemisty 279(23), 24866-24872 (2004). [3]. Stichtenoth, D.O., Thorén, S., Bian, H., et al. Microsomal prostaglandin E synthase is regulated by proinflammatory cytokines and glucocorticoids in primary rheumatoid synovial cells. Journal of Immunology 167, 469-474 (2001). [4]. Guerrero, M.D., Aquino, M., Bruno, I., et al. Synthesis and pharmacological evaluation of a selected library of new potential anti-inflammatory agents bearing the γ-hydroxybutenolide scaffold: a new class of inhibitors of prostanoid production through the selective modulation of microsomal prostaglandin E synthase-1 expression. Journal of Medicinal Chemistry 50, 2176-2184 (2007).