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Merck
모든 사진(1)

주요 문서

T5202

Sigma-Aldrich

TPBM

≥98% (HPLC), solid

동의어(들):

8-Benzylsulfanylmethyl-1,3-dimethyl-3,7-dihydro-purine-2,6-dione, 8-[(Benzylthio)methyl]theophylline, Theophylline, 8-[(benzylthio)methyl]

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About This Item

실험식(Hill 표기법):
C15H16N4O2S
CAS Number:
Molecular Weight:
316.38
MDL number:
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

양식

solid

색상

white to off-white

solubility

DMSO: >5 mg/mL

SMILES string

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

생화학적/생리학적 작용

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.

특징 및 장점

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.

제조 메모

TPBM is soluble in DMSO at a concentration that is greater than 5 mg/ml.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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문서 라이브러리 방문

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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