| Identification | Back Directory | [Name]
CAY10526 | [CAS]
938069-71-7 | [Synonyms]
CAY10526
CAY10526 Exclusive
2(5H)-Furanone, 4-benzo[b]thien-2-yl-3-bromo-5-hydroxy-
3-(1-benzothiophen-2-yl)-4-bromo-2-hydroxy-2H-furan-5-one
WM793,PGE2 production,Inhibitor,inhibit,SB2,microsomal PGE2 synthase-1,A375,cleaved caspase 3,CAY10526,increases apoptosis,increases BAX and BAK,pro-apoptotic,anti-apoptotic,melanoma xenografts,mPGES1 inhibitor,PGE synthase,Prostaglandin E synthase | [Molecular Formula]
C12H7BrO3S | [MDL Number]
MFCD18432686 | [MOL File]
938069-71-7.mol | [Molecular Weight]
311.15 |
| Chemical Properties | Back Directory | [Boiling point ]
561.7±50.0 °C(Predicted) | [density ]
1.889±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 1 mg/ml | [form ]
A crystalline solid | [pka]
8.90±0.60(Predicted) | [color ]
Off-white to yellow | [InChI]
1S/C12H7BrO3S/c13-10-9(11(14)16-12(10)15)8-5-6-3-1-2-4-7(6)17-8/h1-5,11,14H | [InChIKey]
ICCDILPNCJIDAW-UHFFFAOYSA-N | [SMILES]
O=C1OC(C(C2=CC3=C(S2)C=CC=C3)=C1Br)O |
| Hazard Information | Back Directory | [Description]
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). 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. | [Uses]
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]. | [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. DOI:10.1111/pcmr.12455 |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Biokitchen
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| Tel: |
021-021-021-31663258 13795219287 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList20174/0_EN.htm |
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