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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-LM146
LM146

Chemical Structure : LM146

CAS No.: 2767257-95-2

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LM146 (LM-146)

货号: PC-72706Not For Human Use, Lab Use Only.

LM146 (LM-146) is a potent and selective inhibitor of pan-PB1 bromodomains (Polybromo-1 protein, PBRM1 or BAF180), binds to PB1(2), PB1(5), and SMARCA2B with KD values of 110, 61, and 2100 nM, respectively.

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

    生物&药学活性

    LM146 (LM-146) is a potent and selective inhibitor of pan-PB1 bromodomains (Polybromo-1 protein, PBRM1 or BAF180), binds to PB1(2), PB1(5), and SMARCA2B with KD values of 110, 61, and 2100 nM, respectively.
    LM146 displayed 34-fold selectivity profile for PB1(5) over SMARCA2, showed no binding to any bromodomains outside the sub-family VIII at 10 uM.
    PB1 (Polybromo-1 protein) is a component of the BRG1/BRM-associated factor (PBAF) complex, a human analog of the yeast switch/sucrose non-fermenting (SWI/SNF) complex. PB1 is a unique epigenetic reader that contains six distinct bromodomains, while other known bromodomain-containing proteins possess at most two bromodomains. The multi-subunit PBAF complex contains three bromodomain-containing proteins (BCPs): BRD7, a member of the sub-family IV, and SMARCA4 (also known as BRG1) and PB1, two members of the sub-family VIII.

    物理化学性质&存储条件

    分子量 316.829
    分子式 C18H21ClN2O
    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

    6'-Chloro-2-(pentan-3-yl)-1',2'-dihydro-5'H-spiro[cyclopropane-1,3'-pyrrolo[1,2-a]quinazolin]-5'-one

    参考文献

    1. Léa Mélin, et al. ACS Omega. 2021 Aug 9;6(33):21327-21338.

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