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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)
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.
| 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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Product Datasheets for ER 50891
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
If you know of a relevant reference for ER 50891, please let us know.
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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:
Yuan et al (2019) Retinoic Acid Receptor Alpha Represses a Th9 Transcriptional and Epigenomic Program to Reduce Allergic Pathology. Immunity 50 106-120.e10 PMID: 30650370
Centritto et al (2015) Cellular and molecular determinants of all-trans retinoic acid sensitivity in breast cancer: Luminal phenotype and RARα expression. J Reprod Dev 7 950 PMID: 25888236
Jan et al (2022) Controlling neural territory patterning from pluripotency using a systems developmental biology approach. iScience 25 104133 PMID: 35434550
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
Müller et al (2015) Additive Effects of Retinoic Acid (RA) and Bone Morphogenetic Protein 4 (BMP-4) Apoptosis Signaling in Retinoblastoma Cell Lines. PLoS One 10 e0131467 PMID: 26173116
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
Li et al (2017) Diverse feather shape evolution enabled by coupling anisotropic signalling modules with self-organizing branching programme. Nat Commun 8 ncomms14139 PMID: 28106042
Do you know of a great paper that uses ER 50891 from Tocris? Please let us know.
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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
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.