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Chemical Structure : DI-1859
Catalog No.: 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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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.
| M.Wt | 555.782 | |
| Formula | C30H45N5O3S | |
| Appearance | Solid | |
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1. Haibin Zhou, et al. Nat Commun. 2021 May 11;12(1):2621.
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