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]
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关于此项目
经验公式（希尔记法）:
C15H16N4O2S
化学文摘社编号:
分子量:
316.38
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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)
SMILES string
CN1C(=O)N(C)c2nc(CSCc3ccccc3)[nH]c2C1=O
InChI key
FEHAMBYTUPDFJE-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
solid
color
white to off-white
solubility
DMSO: >5 mg/mL
Quality Level
Biochem/physiol Actions
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.
Features and Benefits
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.
Preparation Note
TPBM is soluble in DMSO at a concentration that is greater than 5 mg/ml.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
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
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)
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