Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
DI-591 2245887-38-9 Others DI 591 DI591 inhibitor inhibit