BHPI is an inhibitor (blocker/antagonist) of the nuclear receptor ER_alpha_, which can inhibit cancer/tumor cell protein synthesis and activate the unfolded protein response (UPR).

Physicochemical Properties

Molecular Formula	C21H17NO3
Molecular Weight	331.36458
Exact Mass	331.121
CAS #	56632-39-4
PubChem CID	3860640
Appearance	White to off-white solid powder
LogP	3.777
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	2
Heavy Atom Count	25
Complexity	469
Defined Atom Stereocenter Count	0
InChi Key	FABLAHMQSQFDHR-UHFFFAOYSA-N
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)
Chemical Name	3,3-bis(4-hydroxyphenyl)-7-methyl-1H-indol-2-one
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References

[1]. Estrogen receptor α inhibitor activates the unfolded protein response, blocks protein synthesis, and induces tumor regression. Proc Natl Acad Sci U S A. 2015 Apr 14;112(15):4737-42.

Solubility Data

Solubility (In Vitro)

DMSO : ~120 mg/mL (~362.14 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 3 mg/mL (9.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (9.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.0179 mL	15.0893 mL	30.1787 mL
	5 mM	0.6036 mL	3.0179 mL	6.0357 mL
	10 mM	0.3018 mL	1.5089 mL	3.0179 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.