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:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]9-cis retinoic acid

Ligand Kd (nM):

0.52

Ligand Concentration:

1 nM

Non Specific:

AM580 (1 µM)

Incubation:

120 min at 4°C

Control Inhibitor:

AM580

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 μl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.

Minimum Order Quantity:

2

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

5289501

Name

TTNPB

Measurement

0.7nM - IC50

PubChem ID

24899373

Name

9-cis-Retinoic acid

Measurement

45.9nM - IC50

PubChem ID

10410894

Name

LE 135

Measurement

2885nM - IC50

PubChem ID

2126

Name

AM580

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:

France - Celle L'Evescault

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