| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
DI-1548 (1-1000 nM, 24 hours) inhibited neddylation of cullin 3 in U2OS cells at concentrations as low as 1 nM, with an efficacy approximately 1000 times stronger than DI-591 [1]. DI-1548 (0.3-1000 nM, 24 hours) inhibited neddylation of cullin 3 in various cell lines (including U2OS, MDA-MB-231, KYSE70, and HCT116) and showed selectivity of more than 1000 times for other cullin protein members [1]. DI-1548 (0-1000 nM, 72 hours) showed no cytotoxicity to U2OS, MDA-MB-231, HCT116, and KYSE70 cells at concentrations up to 1000 nM [1]. DI-1548 (30 nM, 0-48 h) can rapidly and persistently selectively inhibit neddylation modification of Cullin 3 (but not Cullin 1)[1]. DI-1548 (0.3-1000 nM, 1 h) selectively and potently stabilizes intracellular DCN1 protein in a dose-dependent manner at nanomolar concentrations, with no significant effect on DCN3[1].
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| ln Vivo |
DI-1548 (25 mg/kg, intraperitoneal injection, single dose) can increase the level of NRF2 protein in C57BL/6 wild-type myocardium[1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: U2OS cells Tested Concentrations: 1, 10, 100 and 1000 nM Incubation Duration: 24 h Experimental Results: Reduced N-Cul3 levels at 1 nM and was approximately 1000 times more potent than DI-591. Western Blot Analysis[1] Cell Types: U2OS, MDA-MB-231, HCT116 and KYSE70 cells Tested Concentrations: 0.3, 1, 3, 10, 30, 100, and 1000 nM Incubation Duration: 24 h Experimental Results: 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. Cell Viability Assay[1] Cell Types: U2OS, MDA-MB-231, HCT116 and KYSE70 cells Tested Concentrations: 0-1000 nM Incubation Duration: 72 h Experimental Results: Showed no cytotoxicity in four cancer cell lines at concentrations up to 1000 nM. Western Blot Analysis[1] Cell Types: U2OS cells Tested Concentrations: 30 nM Incubation Duration: 5 and 30 min,6, 24, and 48 h Experimental Results: 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. Western Blot Analysis[1] Cell Types: U2OS cells Tested Concentrations: 0.3, 1, 3, 10, 30, 100, and 1000 nM Incubation Duration: 1 h Experimental Results: 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. |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 WT mice (~8 weeks) [1]
Doses: 25 mg/kg Route of Administration: i.p., once Experimental Results: 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. |
| References |
| Molecular Formula |
C32H47N5O4S
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|---|---|
| Molecular Weight |
597.81
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| CAS # |
2247060-97-3
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| Appearance |
Typically exists as solids at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6728 mL | 8.3639 mL | 16.7277 mL | |
| 5 mM | 0.3346 mL | 1.6728 mL | 3.3455 mL | |
| 10 mM | 0.1673 mL | 0.8364 mL | 1.6728 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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