ER 50891

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Description: Selective RARα antagonist
Chemical Name: 4-[5-[8-(1-Methylethyl)-4-phenyl-2-quinolinyl]-1H-pyrrolo-2-benzoic acid
Purity: ≥99% (HPLC)
Datasheet
Citations (9)
Reviews
Literature (1)

Biological Activity for ER 50891

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).

Compound Libraries for ER 50891

ER 50891 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for ER 50891

M. Wt 432.51
Formula C29H24N2O2
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 187400-85-7
PubChem ID 10094345
InChI Key LSGNKLDHMQVTEK-UHFFFAOYSA-N
Smiles CC(C)C1=C2C(C(C3=CC=CC=C3)=CC(C4=CC=C(C5=CC=C(C(O)=O)C=C5)N4)=N2)=CC=C1

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.

Solubility Data for ER 50891

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 43.25 100

Preparing Stock Solutions for ER 50891

The following data is based on the product molecular weight 432.51. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.31 mL 11.56 mL 23.12 mL
5 mM 0.46 mL 2.31 mL 4.62 mL
10 mM 0.23 mL 1.16 mL 2.31 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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References for ER 50891

References are publications that support the biological activity of the product.

Kikuchi et al (2001) Syntheses and evaluation of quinoline derivatives as novel retinoic acid receptor α antagonists. Bioorg.Med.Chem.Lett. 11 1215 PMID: 11354380

Ren et al (2005) Impaired retinoic acid (RA) signal leads to RARβ2 epigenetic silencing and RA resistance. Mol.Cell.Biol. 25 10591 PMID: 16287870

Somenzi et al (2007) Disruption of retinoic acid receptor alpha reveals the growth promoter face of retinoic acid. PLoS ONE 9 e836 PMID: 17786207


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Keywords: ER 50891, ER 50891 supplier, ER50891, raralpha, rara, rarα, receptors, antagonists, retinoids, retinoic, acid, selective, Retinoic, Acid, Receptors, 3823, Tocris Bioscience

9 Citations for ER 50891

Citations are publications that use Tocris products. Selected citations for ER 50891 include:

Ning et al (2023) Nuclear receptor modulators inhibit osteosarcoma cell proliferation and tumour growth by regulating the mTOR signaling pathway. Cell Death Dis 14 51 PMID: 36681687

Bi et al (2018) All-trans retinoic-acid inhibits heterodimeric bone morphogenetic protein 2/7-stimulated osteoclastogenesis, and resorption activity. Cell Biosci 8 48 PMID: 30159139

Wang et al (2017) Retinoic acid inhibits white adipogenesis by disrupting GADD45A-mediated Zfp423 DNA demethylation. J Mol Cell Biol 9 338 PMID: 28992291

Olle et al (2017) Testicular organoid generation by a novel in vitro three-layer gradient system. Biomaterials 130 76-89 PMID: 28364632


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Retinoid Receptors Scientific Review

Retinoid Receptors Scientific Review

Written by Alexander Moise, this review summarizes the nature of retinoid receptors, their isotype and isoform variants and modulation of retinoid signaling. Compounds available from Tocris are listed.