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 ActivityLE 135 is a 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).
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Retinobenzoic acids. 6. Retinoid antagonists with heterocyclic ring.
Eyrolles et al.
Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers.
Umemiya et al.
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.
Citations for LE 135
The citations listed below are publications that use Tocris products. Selected citations for LE 135 include:
17 Citations: Showing 1 - 10
All-trans retinoic-acid inhibits heterodimeric bone morphogenetic protein 2/7-stimulated osteoclastogenesis, and resorption activity.
Authors: Bi Et al.
Cell Biosci 2018;8:48
RDH10-mediated retinol metabolism and RARα-mediated retinoic acid signaling are required for submandibular salivary gland initiation.
Authors: Metzler Et al.
Retinoic acid receptor regulation of epimorphic and homeostatic regeneration in the axolotl.
Authors: Nguyen Et al.
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
The Expression of Bone Morphogenetic Protein 2 and Matrix Metalloproteinase 2 through Retinoic Acid Receptor Beta Induced by All-Trans Retinoic Acid in Cultured ARPE-19 Cells.
Authors: Gao Et al.
PLoS One 2016;11:e0150831
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
Additive Effects of Retinoic Acid (RA) and Bone Morphogenetic Protein 4 (BMP-4) Apoptosis Signaling in Retinoblastoma Cell Lines.
Authors: Müller Et al.
PLoS One 2015;10:e0131467
Retinoic acid regulation by CYP26 in vertebrate lens regeneration.
Authors: Thomas and Henry
Cancer Res 2014;386:291
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
The mucosal adjuvant cholera toxin B instructs non-mucosal dendritic cells to promote IgA production via retinoic acid and TGF-β.
Authors: Gloudemans Et al.
PLoS One 2013;8:e59822
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
Retinoic acid induces blood-brain barrier development.
Authors: Mizee Et al.
J Neurosci 2013;33:1660
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
Co-adjuvant effects of retinoic acid and IL-15 induce inflammatory immunity to dietary antigens.
Authors: DePaolo Et al.
Generation of mucosal dendritic cells from bone marrow reveals a critical role of retinoic acid.
Authors: Feng Et al.
J Immunol 2010;185:5915
Retinoids regulate human amniotic tissue-type plasminogen activator gene by a two-step mechanism.
Authors: Borel Et al.
J Cell Mol Med 2010;14:1793
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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