CAY10526

Names

[ Name ]:
CAY10526

[Synonym ]:
4-benzo(b)thiophen-2-yl-3-bromo-5-hydroxy-5H-furan-2-one
4-(1-Benzothiophen-2-yl)-3-bromo-5-hydroxy-2(5H)-furanone
2(5H)-Furanone, 4-benzo[b]thien-2-yl-3-bromo-5-hydroxy-
4-(1-benzothiophen-2-yl)-3-bromo-5-hydroxyfuran-2(5H)-one

Biological Activity

[Description]:

CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanoma cell lines expressing mPGES1[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Immunology/Inflammation >> PGE synthase

[References]

[1]. Sun-Hee Kim, et al. Microsomal PGE2 synthase-1 regulates melanoma cell survival and associates with melanoma disease progression. Pigment Cell Melanoma Res. 2016 May;29(3):297-308.

Chemical & Physical Properties

[ Density]:
1.9±0.1 g/cm3

[ Boiling Point ]:
561.7±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₂H₇BrO₃S

[ Molecular Weight ]:
311.151

[ Flash Point ]:
293.5±30.1 °C

[ Exact Mass ]:
309.929932

[ PSA ]:
74.77000

[ LogP ]:
2.54

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.791