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Submit ReviewBMS 195614
Description: Selective RARα antagonist
Alternative Names: BMS614
Chemical Name: 4-[[[5,6-Dihydro-5,5-dimethyl-8-(3-quinolinyl)-2-naphthalenyl]carbonyl]amino]benzoic acid
Purity: ≥98% (HPLC)
Biological Activity for BMS 195614
BMS 195614 is a neutral retinoic acid receptor (RAR) α-selective antagonist (Ki = 2.5 nM). Displays no significant effect on nuclear receptor corepressor (NCoR) binding; moderately decreases SMRT binding to RAR. Antagonizes agonist-induced coactivator (CoA) recruitment.
Technical Data for BMS 195614
| M. Wt | 448.51 |
| Formula | C29H24N2O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 182135-66-6 |
| PubChem ID | 445091 |
| InChI Key | WGLMBRZXZDAQHP-UHFFFAOYSA-N |
| Smiles | O=C(NC4=CC=C(C(O)=O)C=C4)C3=CC1=C(C=C3)C(C)(C)CC=C1C2=CN=C(C=CC=C5)C5=C2 |
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 BMS 195614
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 11.21 | 25 |
Preparing Stock Solutions for BMS 195614
The following data is based on the product molecular weight 448.51. 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 |
|---|---|---|---|
| 0.25 mM | 8.92 mL | 44.59 mL | 89.18 mL |
| 1.25 mM | 1.78 mL | 8.92 mL | 17.84 mL |
| 2.5 mM | 0.89 mL | 4.46 mL | 8.92 mL |
| 12.5 mM | 0.18 mL | 0.89 mL | 1.78 mL |
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Product Datasheets for BMS 195614
References for BMS 195614
References are publications that support the biological activity of the product.
Gehin et al (1999) Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists. Chem.Biol. 6 519 PMID: 10421757
Germain et al (2009) Differential action on coregulator interaction defines retinoid agonists and neutral antagonists. Chem.Biol. 16 479 PMID: 19477412
Schoenermark et al (1999) Retinoid-mediated suppression of tumor invasion and matrix metalloproteinase synthesis. Ann.N.Y.Acad.Sci. 30 878
If you know of a relevant reference for BMS 195614, please let us know.
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Keywords: BMS 195614, BMS 195614 supplier, BMS195614, retinoic, acid, receptor, RAR, alpha, α, RARa, antagonists, neutral, selective, BMS614, 253310-42-8, Retinoic, Acid, Receptors, 3660, Tocris Bioscience
8 Citations for BMS 195614
Citations are publications that use Tocris products. Selected citations for BMS 195614 include:
Johansson et al (2013) Retinoic acid receptor alpha is associated with tamox. resistance in breast cancer. Nat Commun 4 2175 PMID: 23868472
Flamini et al (2014) Retinoic acid reduces migration of human breast cancer cells: role of retinoic acid receptor beta. J Cell Mol Med 18 1113 PMID: 24720764
Gerald et al (2016) All Trans Retinoic Acid, Transforming Growth Factor β and Prostaglandin E2 in Mouse Plasma Synergize with Basophil-Secreted Interleukin-4 to M2 Polarize Murine Macrophages. PLoS One 11 e0168072 PMID: 27977740
Chen et al (2013) A critical role for the retinoic acid signaling pathway in the pathophysiology of gastrointestinal graft-versus-host disease. Blood 121 3970 PMID: 23529927
Liang et al (2013) Retinoic acid inhibits CD25+ dendritic cell expansion and γδ T-cell activation in experimental autoimmune uveitis. Invest Ophthalmol Vis Sci 54 3493 PMID: 23611991
Mickaël M et al (2020) A Comprehensive Map of the Monocyte-Derived Dendritic Cell Transcriptional Network Engaged upon Innate Sensing of HIV. Cell Rep 30 914-931.e9 PMID: 31968263
Tobias M et al (2019) Retinoic acid worsens ATG10-dependent autophagy impairment in TBK1-mutant hiPSC-derived motoneurons through SQSTM1/p62 accumulation. Autophagy 15 1719-1737 PMID: 30939964
Metzler et al (2018) RDH10-mediated retinol metabolism and RARα-mediated retinoic acid signaling are required for submandibular salivary gland initiation. Development 145 PMID: 29986869
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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.