Physicochemical Properties
| 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
| Targets | USP-1 8.8 nM (IC50) |
| ln Vitro | USP1-IN-9 (20, 100, 500 nM, 24 h) increased the level of monoubiquitinated proliferating cell nuclear antigen (Ub-PCNA) in non-small cell lung cancer (NSCLC) cells in a dose-dependent manner, and USP1-IN-9 also showed an increase in Ub-PCNA at a concentration as low as 20 nM [1]. USP1-IN-9 (0.5 μM, 7 days) significantly inhibited the colony-forming ability of NSCLC cells [1]. USP1-IN-9 (1 nM, 24 h) alone caused a slight cell cycle arrest in olaparib-resistant breast cancer cells, while the combination of olaparib (HY-10162) and USP1-IN-9 caused cell cycle arrest [1]. The combination of USP1-IN-9 (100 nM, 7 days) and olaparib can enhance the killing effect of olaparib on breast cancer cells[1]. |
| ln Vivo | USP1-IN-9 (10 mg/kg, ig) was rapidly absorbed and showed good metabolic stability in male ICR mice[1]. |
| Cell Assay |
Western Blot Analysis[1] Cell Types: NSCLC Tested Concentrations: 20, 100, 500 nM Incubation Duration: 24 h Experimental Results: Elevated the monoubiquitinated PCNA (Ub-PCNA) levels in a dose-dependent manner in NSCLC cells. Cell Viability Assay[1] Cell Types: NSCLC Tested Concentrations: 0.5 nM Incubation Duration: 7 days Experimental Results: Exhibited a substantial inhibition of the colony forming capacity of breast cancer cells compared to the untreated control. Cell Cycle Analysis[1] Cell Types: Breast cancer cells and olaparib-resistant breast cancer Tested Concentrations: 1 nM Incubation Duration: 24 h Experimental Results: Resulted in a minor increase in cells within the S phase, whereas the combination of olaparib and USP1-IN-9 led to an accumulation of cells within the S phase and G2/M phase. Cell Viability Assay[1] Cell Types: Olaparib-resistant breast cancer Tested Concentrations: 100 nM Incubation Duration: 7 days Experimental Results: Alone exhibited a reduction of 30% and did not demonstrate significant cell killing. The inhibition rate of colony formation was further elevated to 50 % combined with USP1-IN-9 and olaparib(100 nM). |
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.) |