BHPI

产品编号 T14553Cas号 56632-39-4

别名

BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression. Elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis. IC50 value: Target: ERα inhibitor BHPI is effective because it elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis. In ERα(+) cancer cells, BHPI rapidly hyperactivates plasma membrane PLCγ, generating inositol 1,4,5-triphosphate (IP3), which opens EnR IP3R calcium channels, rapidly depleting EnR Ca(2+) stores. BHPI distorts a newly described action of estrogen-ERα: mild and transient UPR activation. In contrast, BHPI elicits massive and sustained UPR activation, converting the UPR from protective to toxic.

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BHPI

产品编号 T14553Cas号 56632-39-4

规格	价格	库存
2 mg	¥ 845	5日内发货
5 mg	¥ 1,410	5日内发货
25 mg	¥ 5,820	6-8周
50 mg	¥ 7,570	6-8周
100 mg	¥ 12,400	6-8周
1 mL x 10 mM (in DMSO)	¥ 1,660	5日内发货

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产品介绍

生物活性

产品描述

BHPI is a potent ERα inhibitor that blocks nuclear estrogen–ERα-regulated gene expression effectively. It triggers sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, notably the unfolded protein response (UPR), and consistently inhibits protein synthesis. With an IC50 value targeting ERα, BHPI's mechanism involves the rapid hyperactivation of PLCγ on the plasma membrane in ERα(+) cancer cells, which produces inositol 1,4,5-triphosphate (IP3). This, in turn, opens EnR IP3R calcium channels, leading to a rapid depletion of EnR Ca(2+) stores. SIGNIFICANTLY, BHPI alters estrogen-ERα's usual effect of causing mild and transient UPR activation by inducing a severe and prolonged UPR activation, transforming the UPR from a protective to a toxic response.

偶联与修饰

抗原信息

存储 & 运输

化学信息

分子量	331.36
分子式	C₂₁H₁₇NO₃
CAS No.	56632-39-4

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 150 mg/mL (452.68 mM)

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0179 mL	15.0893 mL	30.1787 mL	150.8933 mL
5 mM	0.6036 mL	3.0179 mL	6.0357 mL	30.1787 mL
10 mM	0.3018 mL	1.5089 mL	3.0179 mL	15.0893 mL
20 mM	0.1509 mL	0.7545 mL	1.5089 mL	7.5447 mL
50 mM	0.0604 mL	0.3018 mL	0.6036 mL	3.0179 mL
100 mM	0.0302 mL	0.1509 mL	0.3018 mL	1.5089 mL