Biological Information

Background Information:

The estrogen-related receptors ERRα, ERRβ, and ERRγ form a subfamily of orphan nuclear receptors that share significant homology with the estrogen receptors ERα and ERβ to possess the potential to positively and negatively regulate estrogen responsiveness. The ER agonist diethylstilbestrol (DES) and the selective ER modulator (SERM) 4-hydroxytamoxifen (4-OHT) have been identified as ERR antagonists. The rational development of synthetic ligands on ERR targets may be useful in improving the treatment of menopause, metabolic disorders, osteoporosis, serum lipids, breast and other cancers.

Family:

NHR

Sub Family:

Estrogen-Related

Class:

Non-Steroid

Protein Name:

ERRbeta

Uniprot Number:

O95718

Gene Name:

ESRRB

Gene ID:

2103

Gene Aliases:

ERR2|ERRbeta|NR3B2|ERRb

Accession Number:

XM_011536547

Organism:

Human

Construct Details:

LBD, Recombinant

Assay Information

Assay Type:

Functional

Assay Sub Type:

Protein-Protein Interaction

Functional Mode:

Antagonist

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Incubation:

1 hr at RT

Control Inhibitor:

4-Hydroxytamoxifen

Criteria For Significance:

≥ 50% decrease in fluorescence relative to GSK4716 response, ≥ 50% increase in fluorescence relative to GSK4716 response

Test Concentration / Dose:

Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM

Test Sample Requirements:

75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)

Minimum Order Quantity:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

448537

Name

Diethylstilbestrol

Measurement

147μM - IC50

PubChem ID

449459

Name

4-Hydroxytamoxifen

Measurement

9.9μM - IC50

PubChem ID

2733526

Name

Tamoxifen

Measurement

90μM - IC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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Item: 311530