LE 135

Catalog # Availability Size / Price Qty
2021/10
2021/50
LE 135 | CAS No. 155877-83-1 | Retinoic Acid Receptor Antagonists
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Description: Selective RARβ antagonist

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

Purity: ≥97%

Product Details
Citations (17)
Reviews

Biological Activity

LE 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).

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. All-trans retinoic-acid inhibits heterodimeric bone morphogenetic protein 2/7-stimulated osteoclastogenesis, and resorption activity
    W Bi, Y Liu, J Guo, Z Lin, J Liu, M Zhou, D Wismeijer, JL Pathak, G Wu
    Cell Biosci, 2018;8(0):48.
  2. Adrenergic beta2 receptor activation stimulates anti-inflammatory properties of dendritic cells in vitro.
    Nijhuis L, Olivier B, Dhawan S, Hilbers F, Boon L, Wolkers M, Samsom J, de Jonge W
    PLoS ONE, 2014;9(1):e85086.
  3. All-trans retinoic acid induces arginase-1 and inducible nitric oxide synthase-producing dendritic cells with T cell inhibitory function.
    Bhatt S, Qin J, Bennett C, Qian S, Fung J, Hamilton T, Lu L
    J Immunol, 2014;192(11):5098-108.
  4. Retinoic acid prevents mesenteric lymph node dendritic cells from inducing IL-13-producing inflammatory Th2 cells.
    Yokota-Nakatsuma A, Takeuchi H, Ohoka Y, Kato C, Song S, Hoshino T, Yagita H, Ohteki T, Iwata M
    Mucosal Immunol, 2014;7(4):786-801.
  5. Retinobenzoic acids. 6. Retinoid antagonists with heterocyclic ring.
    Eyrolles et al.
    J.Med.Chem., 1994;37:1508
  6. Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers.
    Umemiya et al.
    J.Med.Chem., 1997;40:4222
  7. 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
  8. All-trans retinoic acid and human salivary histatin-1 promote the spreading and osteogenic activities of pre-osteoblasts in vitro
    W Sun, A Shi, D Ma, JGM Bolscher, K Nazmi, ECI Veerman, FJ Bikker, H Lin, G Wu
    FEBS Open Bio, 2020;0(0):.

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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

  1. 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
  2. RDH10-mediated retinol metabolism and RARα-mediated retinoic acid signaling are required for submandibular salivary gland initiation.
    Authors: Metzler Et al.
    Development  2018;145
  3. Retinoic acid receptor regulation of epimorphic and homeostatic regeneration in the axolotl.
    Authors: Nguyen Et al.
    Development  2017;144:601
  4. 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
  5. 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
  6. 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
  7. 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
  8. Retinoic acid regulation by CYP26 in vertebrate lens regeneration.
    Authors: Thomas and Henry
    Cancer Res  2014;386:291
  9. 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
  10. 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

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