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Category:
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Nuclear Receptors Retinoic Acid Receptors
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Cat.No.
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Product Name
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2021 |
LE 135
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Price and Availability
Click here for full price details of
LE 135
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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 |
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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
leukaemia cell differentiation induced by Am80 (IC50 = 150 nM).
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
Certificate of Analysis is currently unavailable on-line. Please contact Customer Service
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References:
Eyrolles et al (1994) Retinobenzoic acids. 6. Retinoid antagonists
with heterocyclic ring. J.Med.Chem. 37 1508. Umemiya et
al (1997) Regulation of retinoidal actions by diazepinylbenzoic acids.
Retinoid synergists which activate the RXR-RAR heterodimers. J.Med.Chem. 40
4222. 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.
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or by Research Area
Keywords: LE 135, Retinoic Acid Receptors, RARb-selective Antagonist, LE135, Tocris Bioscience
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