CAY10526

• 常用名: CAY10526
• 英文名: CAY10526
• CAS号: 938069-71-7
• 分子量: 311.151
• 密度: 1.9±0.1 g/cm3
• 沸点: 561.7±50.0 °C at 760 mmHg
• 分子式: C₁₂H₇BrO₃S
• 熔点: N/A
• 闪点: 293.5±30.1 °C

CAY10526用途

CAY10526是一种特异性微粒体PGE2合成酶-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显著抑制黑色素瘤异种移植中的肿瘤生长并增加凋亡。CAY10526降低BCL-2和BCL-XL(抗凋亡)蛋白水平,增加BAX和BAK(促凋亡)以及切割的caspase 3水平。CAY10526抑制表达mPGES1的三种黑色素瘤细胞系的细胞活力(IC50<5μM)[1]。

CAY10526名称

• 英文名: cay10526

CAY10526生物活性

• 描述: CAY10526是一种特异性微粒体PGE2合成酶-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显著抑制黑色素瘤异种移植中的肿瘤生长并增加凋亡。CAY10526降低BCL-2和BCL-XL(抗凋亡)蛋白水平,增加BAX和BAK(促凋亡)以及切割的caspase 3水平。CAY10526抑制表达mPGES1的三种黑色素瘤细胞系的细胞活力(IC50<5μM)[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 免疫及炎症 >> PGE合成酶
• 参考文献:

  [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.

CAY10526物理化学性质

• 密度: 1.9±0.1 g/cm3
• 沸点: 561.7±50.0 °C at 760 mmHg
• 分子式: C₁₂H₇BrO₃S
• 分子量: 311.151
• 闪点: 293.5±30.1 °C
• 精确质量: 309.929932
• PSA: 74.77000
• LogP: 2.54
• InChIKey: ICCDILPNCJIDAW-UHFFFAOYSA-N
• SMILES: O=C1OC(O)C(c2cc3ccccc3s2)=C1Br
• 蒸汽压: 0.0±1.6 mmHg at 25°C
• 折射率: 1.791
• 储存条件: -20°C，密闭，干燥

CAY10526靶点实验

查看更多实验

实验名称：Discovery of Small Molecules to Inhibit Human Cytomegalovirus Nuclear Egress 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：HCMV UL50 External Id：HMS1262

实验名称：Inhibition of pig sPLA2 at 10 uM 来源：ChEMBL 靶标：Phospholipase A2, major isoenzyme External Id：CHEMBL919400

实验名称：Inhibition of human synovial recombinant sPLA2 at 10 uM 来源：ChEMBL 靶标：Phospholipase A2 External Id：CHEMBL919401

实验名称：Inhibition of bee venom sPLA2 at 10 uM 来源：ChEMBL 靶标：Phospholipase A2 External Id：CHEMBL919402

实验名称：Inhibition of PGE2 production in LPS-stimulated mouse RAW264.7 cells at 1 uM after 18... 来源：ChEMBL 靶标：RAW264.7 External Id：CHEMBL919403

实验名称：Antiproliferative activity against human A549 cells assessed as inhibition of cell vi... 来源：ChEMBL 靶标：A549 External Id：CHEMBL4612459

实验名称：Antiproliferative activity against human A549 cells assessed as inhibition of cell vi... 来源：ChEMBL 靶标：A549 External Id：CHEMBL4612458

实验名称：Cell-based high throughput primary assay to identify activators of GPR151 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=G-protein coupled receptor 151; AltName: Full=G-protein coupled receptor PGR7; AltName: Full=GPCR-2037; AltName: Full=Galanin receptor 4; AltName: Full=Galanin-receptor-like protein; Short=GalRL External Id：GPR151_PHUNTER_AG_LUMI_1536_1X%ACT

实验名称：Stabilization of p53 in human papillomavirus-positive cells 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：Cellular tumor antigen p53 External Id：HMS1485

实验名称：Inhibition of Naja naja venom sPLA2 at 10 uM 来源：ChEMBL 靶标：Acidic phospholipase A2 2 External Id：CHEMBL919399

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CAY10526英文别名

• 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
• 4-(1-benzothiophen-2-yl)-3-bromo-5-hydroxyfuran-2(5H)-one