An ERα antagonist
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BHPI

Item No. 17750

Technical Information
Formal Name
1,3-dihydro-3,3-bis(4-hydroxyphenyl)-7-methyl-2H-indol-2-one
CAS Number
56632-39-4
Molecular Formula
C21H17NO3
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMF: 5 mg/mlDMSO: 11 mg/mlEthanol: 14 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
SMILES
CC1=C(NC(C2(C3=CC=C(O)C=C3)C4=CC=C(O)C=C4)=O)C2=CC=C1
InChi Code
InChI=1S/C21H17NO3/c1-13-3-2-4-18-19(13)22-20(25)21(18,14-5-9-16(23)10-6-14)15-7-11-17(24)12-8-15/h2-12,23-24H,1H3,(H,22,25)
InChi Key
FABLAHMQSQFDHR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    BHPI is an antagonist of estrogen receptor α (ERα) that blocks 17β-estradiol-induced proliferation of drug-resistant breast, endometrial, and ovarian cancer cell lines at concentrations ranging from 10 to 1,000 nM.1 It is effective in vivo, driving tumor regression in mice bearing MCF-7 xenografts at a dose of 15 mg/kg daily.1 BHPI specifically inhibits ERα-dependent gene expression and protein synthesis by activating the unfolded protein response in cells.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Andruska, N.D., Zheng, X., Yang, X., et alEstrogen receptor α inhibitor activates the unfolded protein response, blocks protein synthesis, and induces tumor regression. Proc. Natl. Acad. Sci. USA 112(15), 4737-4742 (2015).