TPBM

Names

[ Name ]:
TPBM

[Synonym ]:
tpbm

Biological Activity

[Description]:

TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth[1].

[Related Catalog]:

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Cancer

[Target]

IC50: 9 μM (17β-estradiol (E2)-ERα)[1]

[References]

[1]. Mao C, et al. A new small molecule inhibitor of estrogen receptor alpha binding to estrogen response elements blocks estrogen-dependent growth of cancer cells. J Biol Chem. 2008;283(19):12819-12830.

Chemical & Physical Properties

[ Density]:
1.373g/cm3

[ Boiling Point ]:
569.6ºC at 760mmHg

[ Molecular Formula ]:
C₁₅H₁₆N₄O₂S

[ Molecular Weight ]:
316.37800

[ Flash Point ]:
298.3ºC

[ Exact Mass ]:
316.09900

[ PSA ]:
97.98000

[ LogP ]:
1.39370

[ Index of Refraction ]:
1.661

MSDS

Click to get detail MSDS

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

A noncompetitive small molecule inhibitor of estrogen-regulated gene expression and breast cancer cell growth that enhances proteasome-dependent degradation of estrogen receptor {alpha}.

J. Biol. Chem. 285(53) , 41863-73, (2010)

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....

A new small molecule inhibitor of estrogen receptor alpha binding to estrogen response elements blocks estrogen-dependent growth of cancer cells.

J. Biol. Chem. 283 , 12819-12830, (2008)

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 ...

Related Compounds

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