T5202
TPBM
≥98% (HPLC), solid
别名:
8-Benzylsulfanylmethyl-1,3-dimethyl-3,7-dihydro-purine-2,6-dione, 8-[(Benzylthio)methyl]theophylline, Theophylline, 8-[(benzylthio)methyl]
方案
≥98% (HPLC)
表单
solid
颜色
white to off-white
溶解性
DMSO: >5 mg/mL
SMILES字符串
CN1C(=O)N(C)c2nc(CSCc3ccccc3)[nH]c2C1=O
InChI
1S/C15H16N4O2S/c1-18-13-12(14(20)19(2)15(18)21)16-11(17-13)9-22-8-10-6-4-3-5-7-10/h3-7H,8-9H2,1-2H3,(H,16,17)
InChI key
FEHAMBYTUPDFJE-UHFFFAOYSA-N
生化/生理作用
TPBM is a potent inhibitor of estrogen receptor α via blocking ERα binding to consensus estrogen response element (cERE) DNA.
TPBM is a potent inhibitor of estrogen receptor α via blocking ERα binding to consensus estrogen response element (cERE) DNA. Estrogen receptor α (ERα) plays an important role in several human cancers. Current ERα antagonists bind in the receptor ligand binding pocket and compete for binding with estrogenic ligands. TPBM instead inhibits ERα via binding to consensus estrogen response element (cERE) DNA. TPBM is not toxic to cells and does not effect estrogen-independent cell growth. TPBM does not act by chelating the zinc in ERs zinc fingers and differs from known ERα inhibitors.
特点和优势
This compound is featured on the Nuclear Receptors (Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
制备说明
TPBM is soluble in DMSO at a concentration that is greater than 5 mg/ml.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
Nicole M Kretzer et al.
The Journal of biological chemistry, 285(53), 41863-41873 (2010-11-03)
The mechanisms responsible for 17β-estradiol (E(2))-stimulated breast cancer growth and development of resistance to tamoxifen and other estrogen receptor α (ERα) antagonists are not fully understood. We describe a new tool for dissecting ERα action in breast cancer, p-fluoro-4-(1,2,3,6,-tetrahydro-1,3-dimethyl-2-oxo-6-thionpurin-8-ylthio) (TPSF)
Chengjian Mao et al.
The Journal of biological chemistry, 283(19), 12819-12830 (2008-03-14)
Estrogen receptor alpha (ERalpha) plays an important role in several human cancers. Most current ERalpha antagonists bind in the receptor ligand binding pocket and compete for binding with estrogenic ligands. Instead of the traditional approach of targeting estrogen binding to
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