Physicochemical Properties
| Molecular Formula | C44H58N6O5 |
| Molecular Weight | 750.97 |
| Appearance | Typically exists as solid at room temperature |
| HS Tariff Code | 2934.99.9001 |
| 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) |
Biological Activity
| ln Vitro | Compound 43, proteasome-IN-4, possesses strong antiproliferative properties against MM-1S, RPMI-8226, and MV-4-11 cell lines. Its IC50 values are 15.290, 9.067, and 2.740 nM, respectively, over a 72-hour period (0-20 nM). At concentrations between 10 nM and 1000 nM, proteasome-IN-4 (10-1000 nM; 3 hours) significantly increases the amount of polyubiquitinated proteins[1]. The metabolic stability of proteasome-IN-4 (2μM) in mouse blood is high, with a half-life of 329.21 minutes [1]. |
| ln Vivo | After a one-hour dose in model mice, proteasome-IN-4 (5 mg/kg; iv; single) exhibits superior activity, with intracellular proteasome inhibitory rates of approximately 50%[1]. |
| Cell Assay |
Cell Proliferation Assay Cell Types: MM-1S, RPMI 8226 and MV-4-11 cells[1] Tested Concentrations: 0-20 nM Incubation Duration: 72 hrs (hours) Experimental Results: Displayed potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines, with IC50 of 15.290, 9.067 and 2.740 nM respectively. Western Blot Analysis Cell Types: MM-1S[1] Tested Concentrations: 10, 100 and 1000 nM Incubation Duration: 3 hrs (hours) Experimental Results: Caused massive accumulation of polyubiquitinated proteins at the concentration from 10 nM to 1000 nM. |
| Animal Protocol |
Animal/Disease Models: ICR mice (6-8 weeks) [1] Doses: 5 mg/kg Route of Administration: iv; single Experimental Results: Displayed superior activities with intracellular proteasome inhibitory rates of about 50% after administration of 1 h. |
| References |
[1]. Metabolism guided optimization of peptidomimetics as non-covalent proteasome inhibitors for cancer treatment. Eur J Med Chem. 2022;233:114211. |
Solubility Data
| 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 |
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3316 mL | 6.6581 mL | 13.3161 mL | |
| 5 mM | 0.2663 mL | 1.3316 mL | 2.6632 mL | |
| 10 mM | 0.1332 mL | 0.6658 mL | 1.3316 mL |