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DI-591

Catalog No. T11033   CAS 2245887-38-9

DI-591 is an effective, high-affinity and cell-permeability inhibitor for DCN1-UBC12 interaction. DI-591 binds to DCN1 and DCN2 with Ki values of 12 and nM and 10.4 nM, respectively, and has no obvious binding to DCN3, DCN4 and DCN5 proteins.

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DI-591 Chemical Structure
DI-591, CAS 2245887-38-9
Pack Size Availability Price/USD Quantity
25 mg 8-10 weeks $ 1,420.00
50 mg 8-10 weeks $ 1,850.00
100 mg 8-10 weeks $ 2,970.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description DI-591 is an effective, high-affinity and cell-permeability inhibitor for DCN1-UBC12 interaction. DI-591 binds to DCN1 and DCN2 with Ki values of 12 and nM and 10.4 nM, respectively, and has no obvious binding to DCN3, DCN4 and DCN5 proteins.
In vitro DI-591 binds to DCN1 and DCN2 with Ki values of 12 nM and 10.4 nM, respectively, and has no obvious binding to DCN3, DCN4 and DCN5 proteins. Therefore, DI-591 has a high binding affinity for recombinant human DCN1 and DCN2 proteins, and its selectivity is more than 1000 times that of recombinant human DCN3-5 protein [1]. DI-591 (0-10μM; 1 hour; KYSE70 cells) binds to the DCN1 and DCN2 proteins of the cells and disrupts the binding of the DCN1 and UBC12 proteins. DI-591 (10 μM; 24 hours; THLE2 cells) treatment can strongly increase the mRNA levels of NQO1 and HO1, resulting in the up-regulation of HO1 protein in the cells. It is worth noting that DI-591 has no effect on the mRNA level of NRF2. DI-591's selective inhibition of cullin 3's dienylation leads to the accumulation of NRF2 protein and its transcriptional activation. Knockdown experiments show that DCN1, but not DCN2, plays a key role in the regulation of dimerization of cullin 3 but not other cullins. DI-591 is an excellent probe compound for studying the role of cullin 3 CRL (Cullin-RING E3 ubiquitin ligase) in biological processes and human diseases.
Molecular Weight 585.8
Formula C31H47N5O4S
CAS No. 2245887-38-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Zhou H, et al. A potent small-molecule inhibitor of the DCN1-UBC12 interaction that selectively blocks cullin 3 neddylation. Nat Commun. 2017 Oct 27;8(1):1150.

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Keywords

DI-591 2245887-38-9 Others DI 591 DI591 inhibitor inhibit

 

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