| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ZSNI-21 (48 hours) effectively inhibited the proliferation of Bel-7402, HCC-LM3, RBE, MCF-7 and A549 cancer cells, with IC50 values ranging from 2.399 μM to 5.789 μM, while exhibiting low toxicity to HL-7702 and HEK 293T normal cells [1]. ZSNI-21 can act as a dual inhibitor of ADAM17 and HDAC2, with IC50 values of 0.939 μM and 0.844 μM, respectively, while also effectively inhibiting HDAC6 (IC50 = 0.106 μM) and moderately inhibiting HDAC1 (IC50 = 1.270 μM) [1]. ZSNI-21 (6 hours) showed strong intracellular binding affinity for ADAM17, HDAC1, HDAC2 and HDAC6 in Bel-7402 cells [1]. ZSNI-21 (1.5-12 μM; 48 hours) reduced the level of Notch intracellular domain (NICD) in Bel-7402 cells, increased the level of acetylated histones H3 and H4, regulated apoptosis-related proteins, and reduced the expression of cyclin D1 [1]. ZSNI-21 (3-12 μM; 24 hours) inhibited the long-term proliferation and colony formation of Bel-7402 cells in a concentration-dependent manner [1]. ZSNI-21 (1.5-12 μM; 48 hours) induced apoptosis in Bel-7402 cells in a concentration-dependent manner, manifested by changes in the nuclear morphology of apoptotic cells and an increase in the total apoptosis rate (up to 40.2%) [1]. ZSNI-21 (1.5-6 μM; 48 hours) inhibited the migration of HCC-LM3 cells and reduced the expression of EMT-related proteins in a concentration-dependent manner [1].
|
|---|---|
| ln Vivo |
ZSNI-21 (2000 mg/kg; ig; single dose) showed high in vivo safety in C57BL/6 mice when administered once via gastric administration at a dose of 2000 mg/kg, with no deaths, weight loss or organ damage observed within 14 days [1].
|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: Human hepatocellular carcinoma cells Bel-7402 Tested Concentrations: 1.5 μM; 3 μM; 6 μM; 12 μM Incubation Duration: 48 hours Experimental Results: Concentration-dependently and significantly reduced NICD levels (stronger inhibitory effect than ADAM17 inhibitor JG26). Significantly increased the levels of acetylated histones H3 and H4 (comparable to HDAC inhibitor SAHA). Concentration-dependently downregulated pro-caspase-3 expression. Concentration-dependently downregulated Cyclin D1 expression. Concentration-dependently downregulated Bcl-2 expression. Concentration-dependently upregulated Bax expression. |
| Animal Protocol |
Animal/Disease Models:C57BL/6 (female and male) [1]
Doses: 2000 mg/kg Route of Administration: Gavage; single dose; observation for 14 days Experimental Results: No deaths occurred within 14 days. No significant weight loss occurred within 14 days. No significant pathological changes were observed in the heart, liver, spleen, lungs, and kidneys compared with the control group. |
| References |
| Molecular Formula |
C26H25N3O5
|
|---|---|
| Molecular Weight |
459.49
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
COC(C=C1)=CC=C1OCCN2C(C)=C(C(NC3=CC=C(C(NO)=O)C=C3)=O)C4=C2C=CC=C4
|
| 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)
|
| 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
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 | 2.1763 mL | 10.8816 mL | 21.7633 mL | |
| 5 mM | 0.4353 mL | 2.1763 mL | 4.3527 mL | |
| 10 mM | 0.2176 mL | 1.0882 mL | 2.1763 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.
Products are for research use only; We do not sell to patients
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