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LE 135

Cat. No. 2021

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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 (K_i�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:

438.56

Formula:

C₂₉H₃₀N₂O₂

Solubility:

Soluble to 100 mM in DMSO

Purity:

>97 %

Storage:

Store at +4°C

CAS No:

155877-83-1

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

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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