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Submit ReviewLE 135
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% (HPLC)
Biological Activity for LE 135
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 for LE 135
| M. Wt | 438.56 |
| Formula | C29H30N2O2 |
| Storage | Store at +4°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 155877-83-1 |
| PubChem ID | 10410894 |
| InChI Key | YZZAIQOVMHVWBS-UHFFFAOYSA-N |
| Smiles | CN1C2=C(C=C3C(=C2)C(C)(C)CCC3(C)C)N=C(C2=CC=C(C=C2)C(O)=O)C2=C1C=CC=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 LE 135
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.86 | 100 |
Preparing Stock Solutions for LE 135
The following data is based on the product molecular weight 438.56. 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 |
|---|---|---|---|
| 1 mM | 2.28 mL | 11.4 mL | 22.8 mL |
| 5 mM | 0.46 mL | 2.28 mL | 4.56 mL |
| 10 mM | 0.23 mL | 1.14 mL | 2.28 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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Product Datasheets for LE 135
References for LE 135
References are publications that support the biological activity of the product.
Eyrolles et al (1994) Retinobenzoic acids. 6. Retinoid antagonists with heterocyclic ring. J.Med.Chem. 37 1508 PMID: 8182710
Umemiya et al (1997) Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers. J.Med.Chem. 40 4222 PMID: 9435893
Li et al (1999) 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. J.Biol.Chem. 274 15360 PMID: 10336422
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Keywords: LE 135, LE 135 supplier, Selective, RARβ, RARbeta, antagonists, RAMBA, Retinoic, Acid, Receptors, LE135, 2021, Tocris Bioscience
17 Citations for LE 135
Citations are publications that use Tocris products. Selected citations for LE 135 include:
DePaolo et al (2011) Co-adjuvant effects of retinoic acid and IL-15 induce inflammatory immunity to dietary antigens. Nature 471 220 PMID: 21307853
Bi et al (2018) All-trans retinoic-acid inhibits heterodimeric bone morphogenetic protein 2/7-stimulated osteoclastogenesis, and resorption activity. Cell Biosci 8 48 PMID: 30159139
Cruz et al (2013) High content screening of a kinase-focused library reveals compounds broadly-active against dengue viruses. PLoS Negl Trop Dis 7 e2073 PMID: 23437413
Nguyen et al (2017) Retinoic acid receptor regulation of epimorphic and homeostatic regeneration in the axolotl. Development 144 601 PMID: 28087637
Gloudemans et al (2013) The mucosal adjuvant cholera toxin B instructs non-mucosal dendritic cells to promote IgA production via retinoic acid and TGF-β. PLoS One 8 e59822 PMID: 23527272
Mizee et al (2013) Retinoic acid induces blood-brain barrier development. J Neurosci 33 1660 PMID: 23345238
Müller et al (2015) Additive Effects of Retinoic Acid (RA) and Bone Morphogenetic Protein 4 (BMP-4) Apoptosis Signaling in Retinoblastoma Cell Lines. PLoS One 10 e0131467 PMID: 26173116
Feng et al (2010) Generation of mucosal dendritic cells from bone marrow reveals a critical role of retinoic acid. J Immunol 185 5915 PMID: 20944006
Borel et al (2010) Retinoids regulate human amniotic tissue-type plasminogen activator gene by a two-step mechanism. J Cell Mol Med 14 1793 PMID: 19538480
Duprey-Díaz et al (2016) Exogenous Modulation of Retinoic Acid Signaling Affects Adult RGC Survival in the Frog Visual System afterOptic Nerve Injury PLoS One 11 e0162626 PMID: 27611191
Gao et al (2016) 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. PLoS One 11 e0150831 PMID: 26967733
Thomas and Henry (2014) Retinoic acid regulation by CYP26 in vertebrate lens regeneration. Cancer Res 386 291 PMID: 24384390
Sun et al (2007) Small intestine lamina propria dendritic cells promote de novo generation of Foxp3 T reg cells via retinoic acid. J Exp Med 204 1775 PMID: 17620362
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
Bhatt et al (2014) All-trans retinoic acid induces arginase-1 and inducible nitric oxide synthase-producing dendritic cells with T cell inhibitory function. J Immunol 192 5098 PMID: 24790153
Dhandapani et al (2011) Retinoic acid enhances TRAIL-induced apoptosis in cancer cells by upregulating TRAIL receptor 1 expression. Pharmacol Res Perspect 71 5245 PMID: 21685476
Chen et al (2015) Eosinophils from Murine Lamina Propria Induce Differentiation of Naïve T Cells into Regulatory T Cells via TGF-β1 and Retinoic Acid. Dev Biol 10 e0142881 PMID: 26587591
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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!
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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.