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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-RAR/RXR-LE-540
LE-540

Chemical Structure : LE-540

CAS No.: 188645-44-5

LE-540 (LE 540;LE540)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 488.631
    分子式 C33H32N2O2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    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

    参考文献

    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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