PHTPP

PHTPP is a selective ERβ antagonist.

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Cancer

ERβ[1]

PHTPP is a selective ERβ antagonist. PHTPP reduces FSH-mediated cAMP production by 80% (p<0.01) while it has no effect on basal cAMP[1]. PHTPP (10-6 M) inhibits E2-stimulated ERβ activity, but does not suppress E2-stimulated ERα activity. A high dose of PHTPP (10-6 M) slightly increases class 1 Igf1 mRNA expression, and facilitates the DPN-induced increase in class 1 Igf1 mRNA expression[2].

Cells are plated at a density of 3 to 4×105 in 1 mL of medium per well in a 24-well plate for cell viability and cAMP analysis. Cells are cultured in Dulbecco’s Modified Eagle Medium with PHTPP (1 μM), or ethanol (0.1%) as the vehicle. The incubator is set to an atmosphere of 5% CO2 in air at 37°C, and cultures are allowed to acclimate for at least 24 h. The culture medium is then aspirated and replaced with serum-free DMEM/F12 containing 0.1 μM androstenedione. The cells are collected for intracellular cAMP and to test cell viability[1].

[1]. Compton DR, et al. Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor beta antagonist activity. J Med Chem. 2004 Nov 18;47(24):5872-93.

Elacestrant dihydrochloride | AZD9496 | Kaempferol | XCT 790 | Estrone | GDC-0810 | (20S)-Protopanaxatriol | 27-Hydroxycholesterol | Diethylstilbestrol | 2,3-bis(4-hydroxyphenyl)propionitrile | 4',7-Isoflavandiol | cholesterol | Chrysin | Endoxifen (Z-isomer hydrochloride) | Saikosaponin D