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BMS 195614

Catalog #: 3660
8 Citations Datasheet / COA / SDS
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3660/10
3660/50
BMS 195614 | CAS No. 182135-66-6 | Retinoic Acid Receptor Antagonists
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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%

Product Details
Citations (8)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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

M.Wt:
448.51
Formula:
C29H24N2O3
Solubility:
Soluble to 25 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
182135-66-6

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. Interleukin-22 binding protein (IL-22BP) is constitutively expressed by a subset of conventional dendritic cells and is strongly induced by retinoic acid.
    Martin J, Beriou G, Heslan M, Chauvin C, Utriainen L, Aumeunier A, Scott C, Mowat A, Cerovic V, Houston S, Leboeuf M, Hubert F, Hemont C, Merad M, Milling S, Josien R
    Mucosal Immunol, 2014;7(1):101-13.
  2. All Trans Retinoic Acid, Transforming Growth Factor ? and Prostaglandin E2 in Mouse Plasma Synergize with Basophil-Secreted Interleukin-4 to M2 Polarize Murine Macrophages

    PLoS ONE, 2016;11(12):e0168072.
  3. Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists.
    Gehin et al.
    Chem.Biol., 1999;6:519
  4. Differential action on coregulator interaction defines retinoid agonists and neutral antagonists.
    Germain et al.
    Chem.Biol., 2009;16:479
  5. Retinoid-mediated suppression of tumor invasion and matrix metalloproteinase synthesis.
    Schoenermark et al.
    Ann.N.Y.Acad.Sci., 1999;30:878

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Citations for BMS 195614

The citations listed below are publications that use Tocris products. Selected citations for BMS 195614 include:

8 Citations: Showing 1 - 8

  1. A Comprehensive Map of the Monocyte-Derived Dendritic Cell Transcriptional Network Engaged upon Innate Sensing of HIV.
    Authors: Mickaël M Et al.
    Cell Rep  2020;30:914-931.e9
  2. Retinoic acid worsens ATG10-dependent autophagy impairment in TBK1-mutant hiPSC-derived motoneurons through SQSTM1/p62 accumulation.
    Authors: Tobias M Et al.
    Autophagy  2019;15:1719-1737
  3. RDH10-mediated retinol metabolism and RARα-mediated retinoic acid signaling are required for submandibular salivary gland initiation.
    Authors: Metzler Et al.
    Development  2018;145
  4. 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.
    Authors: Gerald Et al.
    PLoS One  2016;11:e0168072
  5. Retinoic acid reduces migration of human breast cancer cells: role of retinoic acid receptor beta.
    Authors: Flamini Et al.
    J Cell Mol Med  2014;18:1113
  6. Retinoic acid inhibits CD25+ dendritic cell expansion and γδ T-cell activation in experimental autoimmune uveitis.
    Authors: Liang Et al.
    Invest Ophthalmol Vis Sci  2013;54:3493
  7. Retinoic acid receptor alpha is associated with tamox. resistance in breast cancer.
    Authors: Johansson Et al.
    Nat Commun  2013;4:2175
  8. A critical role for the retinoic acid signaling pathway in the pathophysiology of gastrointestinal graft-versus-host disease.
    Authors: Chen Et al.
    Blood  2013;121:3970

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