LE 135

• Supplier: Tocris Bioscience
• Catalog: 4577
• Prices: $149.00, $629.00
• Sizes: 10 mg, 50 mg
• Function Type: Antagonist
• Cas Number: 155877-83-1
• 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)benzoicacid
• Formula: C29H30N2O2
• Molecular Weight: 438.56
• Purity: >97 %
• Description: Retinoic acid antagonist; displays moderate selectivity for RAR β over RAR α (K i values are 0.22 and 1.4 μ M respectively). Highly selective over RAR γ and RXR α . Inhibits human HL-60 leukemia cell differentiation induced by Am80 (IC 50 = 150 nM).

Product References

Retinobenzoic acids. 6. Retinoid antagonists with a heterocyclic ring. - Retinobenzoic acids. 6. Retinoid antagonists with a heterocyclic ring.

Eyrolles L, Kagechika H, Kawachi E, Fukasawa H, Iijima T, Matsushima Y, Hashimoto Y, Shudo K. J Med Chem. 1994 May 13;37(10):1508-17.

Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists - Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists

Umemiya H, Fukasawa H, Ebisawa M, Eyrolles L, Kawachi E, Eisenmann G, Gronemeyer H, Hashimoto Y, Shudo K, Kagechika H. J Med Chem. 1997 Dec 19;40(26):4222-34.

Identification of a novel class of retinoic acid receptor beta-selective retinoid - Identification of a novel class of retinoic acid receptor beta-selective retinoid

Li Y, Hashimoto Y, Agadir A, Kagechika H, Zhang Xk. J Biol Chem. 1999 May 28;274(22):15360-6.