PHTPP has selective antagonism of estrogen ERβ receptor .
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HazMat fee for 500 gram (Estimated)
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ER (Estrogen Receptor) is the receptor of estrogens. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. ER has two receptor subtypes, ERα and ERβ. ERα and ERβ have different tissue distributions and each receptor has similar or unique roles in estrogen-dependent gene expressions.
PHTPP is an selective ERβ antagonist. PHTPP showed a relative binding affinity 36-fold selective for ERβ than ERα[1]. In HEC-1-A cells transfected with estrogen-responsive reporter gene plasmids, 1 μM PHTPP inhibited estrogen stimulated ERβ activity but did not suppress estrogen stimulated ERα activity[2]. 10 μM PHTPP effectively inhibited ERβ transcriptional activity in HEK293 cells transfected with ERβ expressing vector[3]. At the concentrations of 10, 15 and 20 μM, PHTPP dose-dependently inhibited the growth of bladder cancer cells J82, 647v and T24 detected at day 6. J82 cells treated by 20 μM PHTPP had less invasive ability than control group[3].
In a mouse model of BBN-induced bladder cancer, 10 μl of 10 mM PHTPP solution i.p. injected every other day for 12 weeks resulted in smaller tumor masses and better survival rate compared to control group. Moreover, 100% of the mice in the control group developed tumors with muscle invasion while the data was only around 33% in the PHTPP treated group[3].
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