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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-E3 Ubiquitin Ligase-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 Ki of <1 nM, does not bind to DCN3, selectively inhibits neddylation of cullin 3 RING E3 ligase.

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2 mg ￥2480 In stock
5 mg ￥3980 In stock
10 mg ￥5980 In stock
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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, selectively inhibits neddylation of cullin 3 RING E3 ligase.
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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