LE 135

Cat. No. 2021

LE 135 C29H30N2O2 [155877-83-1]

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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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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.

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.

Eyrolles et al (1994) Retinobenzoic acids. 6. Retinoid antagonists with heterocyclic ring. J.Med.Chem. 37 1508. PMID: 8182710.

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Citations are publications that use Tocris products. Selected citations for LE 135 include:

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.

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.

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.

Thomas and Henry (2014) Retinoic acid regulation by CYP26 in vertebrate lens regeneration. Cancer Res 386 291. PMID: 24384390.

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.

DePaolo et al (2011) Co-adjuvant effects of retinoic acid and IL-15 induce inflammatory immunity to dietary antigens. Nature 471 220. PMID: 21307853.

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.

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.

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.

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Keywords: LE 135, supplier, Selective, RARβ, RARbeta, antagonists, RAMBA, Retinoic, Acid, Receptors, LE135, Tocris Bioscience, Retinoic Acid Receptor Antagonist products

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