DI-1548
Based on 1 Customer Validation
DI-1548 is a potent, selective, and irreversible covalent inhibitor of DCN1 (IC50 = 4.6 nM). DI-1548 potently and selectively inhibits cullin 3 neddylation at nanomolar concentrations, and exhibits no obvious effect on the neddylation of other cullin members (including cullin 1, 2, 4A, 4B, and 5). DI-1548 exhibits no cytotoxicity. DI-1548 covalently binds to DCN1, disrupting the DCN1-UBC12 interaction, causing the collapse of the neddylation complex, inactivating CRL3, leading to NRF2 accumulation and upregulation of its target genes, and ultimately protecting mice from liver damage. DI-1548 can be used in liver injury research.
For research use only. We do not sell to patients.
- Purity : 99.40%
- CAS No.: 2247060-97-3
- Formula: C32H47N5O4S
- Molecular Weight:597.81
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
DI-1548 (1-1000 nM, 24 h) inhibits cullin 3 neddylation at concentrations as low as 1 nM and are approximately 1000 times more potent than DI-591 (HY-124602) in U2OS cells[1].
DI-1548 (0.3-1000 nM, 24 h) inhibits the neddylation of cullin 3 with over 1000-fold selectivity over other cullin members in various cell lines, including U2OS, MDA-MB-231, KYSE70, and HCT116[1].
DI-1548 (0-1000 nM, 72 h) shows no cytotoxicity in U2OS, MDA-MB-231, HCT116 and KYSE70 cells at concentrations up to 1000 nM[1].
DI-1548 (30 nM, 0-48 h) has fast kinetics in selective inhibition of the neddylation of cullin 3 over cullin 1[1].
DI-1548 (0.3-1000 nM, 1 h) selectively and potently stabilizes cellular DCN1 in a dose-dependent manner at nanomolar concentrations, with no observable effect on DCN3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U2OS cells
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Concentration:1, 10, 100 and 1000 nM
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Incubation Time:24 h
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Result:Reduced N-Cul3 levels at 1 nM and was approximately 1000 times more potent than DI-591.
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Cell Line:U2OS, MDA-MB-231, HCT116 and KYSE70 cells
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Concentration:0.3, 1, 3, 10, 30, 100, and 1000 nM
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Incubation Time:24 h
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Result:Significantly reduced the level of N-CUL3 at concentrations as low as 0.3 nM, and achieved profound inhibition of the neddylation of cullin 3 at 1-3 nM.
Demonstrate over 300-fold greater potency than DI-591 across various cell lines.
Had no obvious effect on the neddylation of other cullin members that were examined, including cullin 1, 2, 4A, 4B, and 5 at concentrations up to 1000 nM.
Induced significant accumulation of NRF2 protein at concentrations as low as 0.3-1 nM, and was 100-1000 times more potent than DI-591.
Had no obvious effect on protein levels of KEAP1 and p62 in U2OS cells.
Had no effect on the levels of p21 and BIM proteins, substrates of CRL1, and CDT1, a substrate of CRL4A, at concentrations up to 1000 nM, consistent with its inability to inhibit neddylation of these cullin members.
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Cell Line:U2OS, MDA-MB-231, HCT116 and KYSE70 cells
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Concentration:0-1000 nM
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Incubation Time:72 h
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Result:Showed no cytotoxicity in four cancer cell lines at concentrations up to 1000 nM.
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Cell Line:U2OS cells
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Concentration:30 nM
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Incubation Time:5 and 30 min,6, 24, and 48 h
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Result:Inhibited the neddylation of cullin 3 within 5min but had no effect on the neddylation of cullin 1 with treatment time up to 48 h.
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Cell Line:U2OS cells
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Concentration:0.3, 1, 3, 10, 30, 100, and 1000 nM
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Incubation Time:1 h
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Result:Enhanced the thermal stability of DCN1 protein in a dose-dependent manner at concentrations as low as 0.3 nM.
Exhibited over 1000-fold greater potency than DI-591 in enhancing the thermal stability of cellular DCN1 protein.
Showed no discernible effect on the thermal stability of cellular DCN3 protein at concentrations up to 1000 nM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 WT mice (~8 weeks) [1]
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Dosage:25 mg/kg
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Administration:i.p., once
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Result:Induced robust upregulation of NRF2 protein in the mouse liver.
Produced a sustained PD effect in the liver despite being cleared from systemic circulation within 3 hours.
Chemical Information
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CAS No. 2247060-97-3
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Appearance Solid
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Molecular Weight 597.81
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Formula C32H47N5O4S
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Color White to off-white
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SMILES
C=C(CN1CCOCC1)C(NC[C@H](C2CCCCC2)NC([C@@H](NC(CC)=O)CC(SC3=C4)=NC3=CC=C4C(C)C)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (167.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Hot Topics
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All
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Topics
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Most Recent
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Oldest
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Topics Protein Neddylation: Pathophysiology to Therapy
Protein neddylation is a ubiquitin-like post-translational modification in which NEDD8 is enzymatically conjugated to lysine residues on substrate proteins, thereby regulating protein activity, stability, conformation, and complex assembly.
2026-06-18
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.6728 mL | 8.3639 mL | 16.7277 mL | 41.8193 mL |
| 5 mM | 0.3346 mL | 1.6728 mL | 3.3455 mL | 8.3639 mL | |
| 10 mM | 0.1673 mL | 0.8364 mL | 1.6728 mL | 4.1819 mL | |
| 15 mM | 0.1115 mL | 0.5576 mL | 1.1152 mL | 2.7880 mL | |
| 20 mM | 0.0836 mL | 0.4182 mL | 0.8364 mL | 2.0910 mL | |
| 25 mM | 0.0669 mL | 0.3346 mL | 0.6691 mL | 1.6728 mL | |
| 30 mM | 0.0558 mL | 0.2788 mL | 0.5576 mL | 1.3940 mL | |
| 40 mM | 0.0418 mL | 0.2091 mL | 0.4182 mL | 1.0455 mL | |
| 50 mM | 0.0335 mL | 0.1673 mL | 0.3346 mL | 0.8364 mL | |
| 60 mM | 0.0279 mL | 0.1394 mL | 0.2788 mL | 0.6970 mL | |
| 80 mM | 0.0209 mL | 0.1045 mL | 0.2091 mL | 0.5227 mL | |
| 100 mM | 0.0167 mL | 0.0836 mL | 0.1673 mL | 0.4182 mL |
DI-1548 Related Classifications
HY-156240 Related Classifications
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