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LE135

Chemical Structure : LE135

CAS No.: 155877-83-1

LE135 (LE-135)

Catalog No.: PC-20199Not For Human Use, Lab Use Only.

LE135 is a retinoic acid receptor (RAR) antagonist that displays moderate selectivity for RARβ over RARα (Ki values=0.22 and 1.4 μM, respectively), highly selective over RARγ and RXRα.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

LE135 is a retinoic acid receptor (RAR) antagonist that displays moderate selectivity for RARβ over RARα (Ki values=0.22 and 1.4 μM, respectively), highly selective over RARγ and RXRα.
LE135 inhibited retinoic acid (RA)-induced transcriptional activation of RARbeta, but not RARalpha, RARgamma or retinoid X receptor alpha (RXRalpha), on a variety of RA response elements.
LE135 inhibited all-trans-RA-induced apoptosis in ZR-75-1 human breast cancer cells.

Physicochemical Properties

M.Wt 438.57
Formula C29H30N2O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(5,7,7,10,10-pentamethyl-7,8,9,10-tetrahydro-5H-benzo[e]naphtho[2,3-b][1,4]diazepin-13-yl)benzoic acid

References

1. Li Y, et al. J Biol Chem. 1999 May 28;274(22):15360-6.

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