Catalog Number: 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 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:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
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.
Background References
  1. Retinobenzoic acids. 6. Retinoid antagonists with heterocyclic ring.
    Eyrolles et al.
    J.Med.Chem., 1994;37:1508
  2. Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers.
    Umemiya et al.
    J.Med.Chem., 1997;40:4222
  3. 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.
    Li et al.
    J.Biol.Chem., 1999;274:15360
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