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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Ubiquitin-conjugating Enzyme (E2)-DI-1859
DI-1859

Chemical Structure : DI-1859

CAS No.: 2247061-09-0

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DI-1859 (DI 1859)

货号: PC-72231Not For Human Use, Lab Use Only.

DI-1859 (DI 1859) is a potent, selective and covalent DCN1 inhibitor with IC50 of 4.6 nM and Ki of <1 nM, does not bind to DCN3.

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

    生物&药学活性

    DI-1859 (DI 1859) is a potent, selective and covalent DCN1 inhibitor with Ki of <1 nM, does not bind to DCN3.
    DI-1859 could inhibit cullin 3 neddylation at concentration as low as 1 nM, which is 1000 times more potent than DI-591.
    DI-1859 selectively inhibits neddylation of cullin 3 in cells at low nanomolar concentrations and are 2-3 orders of magnitude more potent than our previously reported reversible DCN1 inhibitor DI-591.
    DI-1859 at concentrations as low as 0.3 nM significantly reduced the level of neddylated cullin 3 and achieve profound inhibition of the neddylation of cullin 3 at 1-3 n.
    DI-1859 is ~30 times more potent than MLN4924 in inhibition of the neddylation of cullin 3 in THLE2 liver cells.
    DI-1859 induced a robust increase of NRF2 protein, a CRL3 substrate, in mouse liver and effectively protected mice from acetaminophen-induced liver damage.

    物理化学性质&存储条件

    分子量 555.782
    分子式 C30H45N5O3S
    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

    N-((S)-2-cyclohexyl-2-((S)-3-(6-isopropylbenzo[d]thiazol-2-yl)-2-propionamidopropanamido)ethyl)-2-((dimethylamino)methyl)acrylamide

    参考文献

    1. Haibin Zhou, et al. Nat Commun. 2021 May 11;12(1):2621.

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