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DIZ-3 2675490-72-7

DIZ-3 2675490-72-7

CAS No.: 2675490-72-7

DIZ-3 is a selective multimeric G4 ligand based on a G4 ligand dimerization strategy. DIZ-3 is inserted into the G4-G4 i
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DIZ-3 is a selective multimeric G4 ligand based on a G4 ligand dimerization strategy. DIZ-3 is inserted into the G4-G4 interface to stabilize the high-order structure. DIZ-3 induces cell cycle arrest and apoptosis, thereby inhibiting cell proliferation/growth in alternative elongation of telomeres (ALT) in cancer cells.

Physicochemical Properties


CAS # 2675490-72-7
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 DIZ-3 (0-40 μM; 24 hours) prevents the spread of cancer cell lines associated with ALT [1]. In U2OS, DIZ-3 (0.6-2.5 μM; 24 hours) causes apoptosis and cell cycle arrest [1]. DIZ-3 (0.12, 0.25, 0.5 μM; 7 days) induces the development of U2OS cell colonies [1]. The migration of U2OS cells is considerably inhibited by DIZ-3 (0.12, 0.25, 0.5 μM; 24 hours) [1].
Cell Assay Cell Proliferation Assay[1]
Cell Types: Human bone osteosarcoma U2OS cells, normal BJ fibroblasts
Tested Concentrations: 0-40 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: Caused a significant dose-dependent cytotoxic effect on U2OS cancer cells with an IC50 of 2.1 µM. Induced much weaker growth inhibition on normal BJ fibroblasts with an IC50 of 29.3 µM.

Apoptosis Analysis[1]
Cell Types: U2OS cells
Tested Concentrations: 0.6, 1.2, 2.5 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: Induced significant apoptosis in U2OS cells (the percentage of apoptotic cells increased from 10.1% to 24.9%).

Cell Cycle Analysis[1]
Cell Types: U2OS cells
Tested Concentrations: 0.6, 1.2, 2.5 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: Induced the apparent accumulation of cells in the S phase (increasing from 24.0% to 32.2%) in a dose-dependent manner.
References

[1]. Dimeric aryl-substituted imidazoles may inhibit ALT cancer by targeting the multimeric G-quadruplex in telomere. Eur J Med Chem. 2020 Jan 15;186:111891.


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.)