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LE-540

Chemical Structure : LE-540

CAS No.: 188645-44-5

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LE-540 (LE 540;LE540)

Catalog No.: PC-70292Not For Human Use, Lab Use Only.

LE-540 (LE540) is a potent, selective RARβ antagonist that inhibits RA-induced transcriptional activation of RARβ, but not RARα, RARγ or RXRα on a variety of RA response elements.

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

    Biological Activity

    LE-540 (LE540) is a potent, selective RARβ antagonist that inhibits RA-induced transcriptional activation of RARβ, but not RARα, RARγ or RXRα on a variety of RA response elements.
    LE-540 inhibits ATRA-induced apoptosis in ZR-75-1 human breast cancer cells.
    LE-540 strongly represses 12-O-tetradecanoylphorbol-13-acetate-induced AP-1 activity in the presence of RARβ and RARα.

    Physicochemical Properties

    M.Wt 488.631
    Formula C33H32N2O2
    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-(10,10,13,13,15-pentamethyl-11,12,13,15-tetrahydro-10H-dinaphtho[2,3-b:1',2'-e][1,4]diazepin-7-yl)benzoic acid

    References

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

    2. Kitaoka K, et al. Brain Res. 2011 Nov 14;1423:10-6.

    3. Umemiya H, et al. J Med Chem. 1997 Dec 19;40(26):4222-34.

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