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

Soluble to 100 mM in DMSO
>97 %
Store at +4°C

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 / Safety Data Sheet

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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, supplier, Selective, RARβ, RARbeta, antagonists, RAMBA, Retinoic, Acid, Receptors, LE135, Retinoic Acid Receptor Antagonists

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