ER 50891

Catalog # Availability Size / Price Qty
3823/10
3823/50
ER 50891 | CAS No. 187400-85-7 | Retinoic Acid Receptor Antagonists
1 Image
Description: Selective RARα antagonist

Chemical Name: 4-[5-[8-(1-Methylethyl)-4-phenyl-2-quinolinyl]-1H-pyrrolo-2-benzoic acid

Purity: ≥99%

Product Details
Citations (9)
Reviews

Biological Activity

ER 50891 is an antagonist of RARα receptors (IC50 = 31.2 nM). Displays selective affinity for RARα (relative IC50 values are 1.8, 432 and 535 nM for RARα, RARγ and RARβ respectively).

Technical Data

M.Wt:
432.51
Formula:
C29H24N2O2
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥99%
Storage:
Store at RT
CAS No:
187400-85-7

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Retinoids induce integrin-independent lymphocyte adhesion through RAR-alpha nuclear receptor activity.
    Whelan J, Wang L, Chen J, Metts M, Nasser T, McGoldrick L, Bridges L
    Biochem Biophys Res Commun, 2014;454(4):537-542.
  2. All-trans retinoic-acid inhibits heterodimeric bone morphogenetic protein 2/7-stimulated osteoclastogenesis, and resorption activity
    W Bi, Y Liu, J Guo, Z Lin, J Liu, M Zhou, D Wismeijer, JL Pathak, G Wu
    Cell Biosci, 2018;8(0):48.
  3. Syntheses and evaluation of quinoline derivatives as novel retinoic acid receptor α antagonists.
    Kikuchi et al.
    Bioorg.Med.Chem.Lett., 2001;11:1215
  4. Impaired retinoic acid (RA) signal leads to RARβ2 epigenetic silencing and RA resistance.
    Ren et al.
    Mol.Cell.Biol., 2005;25:10591
  5. Disruption of retinoic acid receptor alpha reveals the growth promoter face of retinoic acid.
    Somenzi et al.
    PLoS ONE, 2007;9:e836
  6. All-trans retinoic acid and human salivary histatin-1 promote the spreading and osteogenic activities of pre-osteoblasts in vitro
    W Sun, A Shi, D Ma, JGM Bolscher, K Nazmi, ECI Veerman, FJ Bikker, H Lin, G Wu
    FEBS Open Bio, 2020;0(0):.

Product Datasheets

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Citations for ER 50891

The citations listed below are publications that use Tocris products. Selected citations for ER 50891 include:

9 Citations: Showing 1 - 9

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