Cat. No. 2021
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 ActivityRetinoic 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).
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
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
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