Date published: 2026-3-3

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GPR30 Inhibitors

GPR30 inhibitors represent a class of chemical compounds designed to selectively target and modulate the activity of the G protein-coupled estrogen receptor 30 (GPR30). These inhibitors play a crucial role in unraveling the intricate signaling pathways associated with GPR30 and understanding its functional significance in diverse cellular processes. One prominent class of GPR30 inhibitors includes small molecules such as G-15, G15-DHP, and G36, which directly bind to GPR30, preventing its activation and subsequent signaling cascades. These inhibitors disrupt pathways like the cAMP/PKA, MAPK, and PI3K/Akt, offering researchers precise tools to investigate GPR30-mediated cellular responses. Tamoxifen and Fulvestrant, known for their roles as estrogen receptor modulators and degraders, respectively, also exhibit inhibitory effects on GPR30. They interfere with estrogen receptor interactions, indirectly influencing GPR30 signaling pathways and providing valuable insights into the cross-talk between estrogen receptors. Additionally, compounds like OHTDS and GPR30 Inhibitor 1 demonstrate specificity for GPR30, influencing its activity and downstream pathways. These inhibitors contribute to our understanding of the nuanced roles of GPR30 in cellular processes and offer avenues for interventions.

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Estriol

50-27-1sc-205682
sc-205682A
100 mg
500 mg
$21.00
$65.00
(0)

Estriol functions as a GPR30 inhibitor, characterized by its selective binding affinity that engages in specific electrostatic interactions with the receptor's active site. This compound demonstrates a rapid kinetic profile, facilitating quick receptor occupancy and subsequent modulation of downstream signaling pathways. Its unique three-dimensional structure allows for distinct conformational changes in GPR30, potentially influencing cellular responses and regulatory mechanisms. The compound's solubility properties further enhance its interaction dynamics within biological systems.

GSK 4716

101574-65-6sc-203986
sc-203986A
10 mg
50 mg
$71.00
$285.00
(1)

GSK4716 is a GPR30 antagonist that competes with endogenous ligands for binding to the receptor. This competition results in the inhibition of GPR30-mediated signaling pathways, particularly the cAMP/PKA and PI3K/Akt pathways. GSK4716's mechanism of action involves disrupting the normal activation of GPR30, making it a reliable chemical for investigating the functional roles of GPR30 in various cellular contexts.

ICI 182,780

129453-61-8sc-203435
sc-203435A
1 mg
10 mg
$83.00
$187.00
34
(1)

Fulvestrant, classified as a selective estrogen receptor degrader (SERD), indirectly inhibits GPR30. By promoting the degradation of estrogen receptors, including GPR30, Fulvestrant reduces the availability of functional receptors for activation. This results in a comprehensive attenuation of GPR30-mediated signaling cascades, impacting pathways such as PI3K/Akt and ERK1/2. Fulvestrant's dual mechanism offers insights into the intricate regulation of estrogen signaling pathways.

β-Estradiol

50-28-2sc-204431
sc-204431A
500 mg
5 g
$63.00
$182.00
8
(1)

While traditionally recognized as an estrogen hormone, estradiol can also exert antagonist effects on GPR30. In certain contexts, high concentrations of estradiol can compete with endogenous ligands for GPR30 binding, leading to the inhibition of its normal activation. This results in the modulation of GPR30-mediated signaling pathways, including the regulation of cAMP/PKA and calcium signaling, highlighting the intricate dual role of estradiol in estrogen receptor modulation.

GSK 429286

864082-47-3sc-361200
sc-361200B
sc-361200A
1 mg
5 mg
10 mg
$40.00
$125.00
$235.00
(1)

GPR30 Inhibitor 1 is a small molecule antagonist designed to specifically target and inhibit GPR30. By binding to the receptor, this inhibitor disrupts GPR30-mediated signaling pathways, affecting downstream effectors such as MAPK and PI3K/Akt. The compound's design ensures high selectivity for GPR30, making it a valuable tool in elucidating the nuanced roles of GPR30 in various cellular processes and its potential implications in health and disease.

(Z)-4-Hydroxytamoxifen

68047-06-3sc-3542C
sc-3542
sc-3542B
sc-3542A
sc-3542D
sc-3542E
1 mg
5 mg
10 mg
25 mg
50 mg
100 mg
$220.00
$281.00
$408.00
$718.00
$1377.00
$2397.00
20
(2)

GPR30 Inhibitor 2 is a chemical compound designed for the specific inhibition of GPR30. Its mechanism involves interfering with the receptor's activation and subsequent downstream signaling. This inhibitor particularly impacts GPR30-mediated pathways like cAMP/PKA and MAPK. The structural features of GPR30 Inhibitor 2 contribute to its selectivity, making it an essential tool for researchers investigating the molecular intricacies of GPR30 function in diverse cellular contexts.