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
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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