Catalog Number: 2021
Chemical Name: 4-(7,8,9,10-Tetrahydro-5,7,7,10,10-pentamethyl-5H-benzo[e]naphtho[2,3-b][1,4]diazepin-13-yl)benzoic acid
Biological Activity
Retinoic acid antagonist; displays moderate selectivity for RARβ over RARα (Ki�values are 0.22 and 1.4 μM respectively). Highly selective over RARγ and RXRα. Inhibits human HL-60 leukemia cell differentiation induced by Am80 (IC50 = 150 nM).
Technical Data
  • M.Wt:
    438.56
  • Formula:
    C29H30N2O2
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >97%
  • Storage:
    Store at +4°C
  • CAS No:
    155877-83-1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Retinobenzoic acids. 6. Retinoid antagonists with heterocyclic ring.
    Eyrolles et al.
    J.Med.Chem., 1994;37:1508
  2. Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers.
    Umemiya et al.
    J.Med.Chem., 1997;40:4222
  3. Identification of a novel class of retinoic acid receptor β-selective retinoid antagonists and their inhibitory effects on AP-1 activity and retinoic acid-induced apoptosis in human breast cancer cells.
    Li et al.
    J.Biol.Chem., 1999;274:15360
Citations:

The citations listed below are publications that use Tocris products. Selected citations for LE 135 include:

9 Citations: Showing 1 - 9
Filter your results:

  1. Exogenous Modulation of Retinoic Acid Signaling Affects Adult RGC Survival in the Frog Visual System afterOptic Nerve Injury
    Authors: Duprey-Díaz Et al.
    PLoS One 2016;11:e0162626
  2. Eosinophils from Murine Lamina Propria Induce Differentiation of Naïve T Cells into Regulatory T Cells via TGF-β1 and Retinoic Acid.
    Authors: Chen Et al.
    Dev Biol 2015;10:e0142881
  3. Retinoic acid regulation by CYP26 in vertebrate lens regeneration.
    Authors: Thomas and Henry
    Cancer Res 2014;386:291
  4. All-trans retinoic acid induces arginase-1 and inducible nitric oxide synthase-producing dendritic cells with T cell inhibitory function.
    Authors: Bhatt Et al.
    J Immunol 2014;192:5098
  5. High content screening of a kinase-focused library reveals compounds broadly-active against dengue viruses.
    Authors: Cruz Et al.
    PLoS Negl Trop Dis 2013;7:e2073
  6. Retinoic acid enhances TRAIL-induced apoptosis in cancer cells by upregulating TRAIL receptor 1 expression.
    Authors: Dhandapani Et al.
    Pharmacol Res Perspect 2011;71:5245
  7. Co-adjuvant effects of retinoic acid and IL-15 induce inflammatory immunity to dietary antigens.
    Authors: DePaolo Et al.
    Nature 2011;471:220
  8. Generation of mucosal dendritic cells from bone marrow reveals a critical role of retinoic acid.
    Authors: Feng Et al.
    J Immunol 2010;185:5915
  9. Small intestine lamina propria dendritic cells promote de novo generation of Foxp3 T reg cells via retinoic acid.
    Authors: Sun Et al.
    J Exp Med 2007;204:1775

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