Biological Information

Background Information:

Retinoic acid receptors (RARs) are retinoic acid inducible enhancer factors belonging to the superfamily of steroid/thyroid receptors. The retinoic acid metabolite has profound effects on vertebrate development. Retinoic acid is a morphogen and a powerful tetragen. This receptor controls cell function by directly regulating gene expression. Inhibition of RARA (RAR α, NR1B1) may be useful in the treatment of various cancers.

Family:

NHR

Sub Family:

Retinoic Acid

Class:

Non-Steroid

Protein Name:

RARalpha

Uniprot Number:

P10276

Protein Aliases:

Nuclear receptor subfamily 1 group B member 1

Gene Name:

RARA

Gene ID:

5914

Gene Aliases:

RAR|NR1B1

Accession Number:

XM_017024920

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:

16 hr at 4°C

Control Inhibitor:

Ro41-5253

Criteria For Significance:

≥ 50% increase in fluorescence relative to TTNPB response, ≥ 50% Inhibition of TTNPB-induced fluorescence

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

5312120

Name

LG-629

Measurement

4.1nM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Adverse / Beneficial Action:

Inhibition of RARA (RAR , NR1B1) may be useful in the treatment of various cancers.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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