2. NF-κB Apoptosis
  3. NF-κB Apoptosis
  4. DCZ0415

DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients.

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DCZ0415 Chemical Structure

DCZ0415 Chemical Structure

CAS No. : 2242470-43-3

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Based on 4 publication(s) in Google Scholar

DCZ0415 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients[1].

IC50 & Target[1]

NF-κB

 

In Vitro

DCZ0415 (10, 20 μM; 72 hours) shows a significant decrease in colony formation, indicating it inhibits cell proliferation[1].
DCZ0415 (1.25-40 μM; 72 hours) induces a significant dose-dependent decrease of viability in MM cells[1].
DCZ0415 (10, 20 μM; 24-72 hours) shows a dose-dependent relationship between DCZ0415 treatment and apoptotic cell death[1].
DCZ0415 (10, 20 μM; 24 hours) induces a significant accumulation in G0/G1 MM cells[1].
DCZ0415 (10 μM; 48 hours) decreases the protein levels of phosphorylated (p)-iκBα and phosphorylated (p)-NF-κB in MM cells[1].
DCZ0415 has IC50s of 1.0–10 μM in CalcuSyn in MM cell lines[1].
DCZ0415 exerts cytotoxic effects by inhibiting DNA 288 synthesis in MM cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

DCZ0415 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Multiple myeloma (MM) cells
Concentration: 10, 20 μM
Incubation Time: 72 hours
Result: Showed a significant decrease in colony formation, indicating it inhibits cell proliferation.

Cell Viability Assay[1]

Cell Line: MM cells
Concentration: 1.25, 2.5, 5, 10, 20, 40 μM
Incubation Time: 72 hours
Result: Induced a significant dose-dependent decrease of viability.

Apoptosis Analysis[1]

Cell Line: MM cells
Concentration: 10, 20 μM
Incubation Time: 24, 48, 72 hours
Result: Showed a dose-dependent relationship between DCZ0415 treatment and apoptotic cell death.

Cell Cycle Analysis[1]

Cell Line: MM cells
Concentration: 10 and 20 μM
Incubation Time: 24 hours
Result: Induced a significant accumulation in G0/G1 MM cells.

Western Blot Analysis[1]

Cell Line: MM cells
Concentration: 10 μM
Incubation Time: 48 hours
Result: Decreased the protein levels of phosphorylated (p)-iκBα and phosphorylated (p)-NF-κB in MM cells.
In Vivo

DCZ0415 (ip; 50 mg/kg/day for 14 days) significantly reduces the growth of MM cells-induced tumors in immune-deficient mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice (6-weeks-old) with H929 775 cells[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; every day for 14 days
Result: Significantly reduced the growth of MM cells-induced tumors.
Molecular Weight

356.42

Formula

C23H20N2O2
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C1N(C2=CC=C(CC3=CC=NC=C3)C=C2)C(C4C5C(C6)C6C(C=C5)C14)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (175.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8057 mL 14.0284 mL 28.0568 mL
5 mM 0.5611 mL 2.8057 mL 5.6114 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.77%

COA (249 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8057 mL 14.0284 mL 28.0568 mL 70.1420 mL
5 mM 0.5611 mL 2.8057 mL 5.6114 mL 14.0284 mL
10 mM 0.2806 mL 1.4028 mL 2.8057 mL 7.0142 mL
15 mM 0.1870 mL 0.9352 mL 1.8705 mL 4.6761 mL
20 mM 0.1403 mL 0.7014 mL 1.4028 mL 3.5071 mL
25 mM 0.1122 mL 0.5611 mL 1.1223 mL 2.8057 mL
30 mM 0.0935 mL 0.4676 mL 0.9352 mL 2.3381 mL
40 mM 0.0701 mL 0.3507 mL 0.7014 mL 1.7535 mL
50 mM 0.0561 mL 0.2806 mL 0.5611 mL 1.4028 mL
60 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1690 mL
80 mM 0.0351 mL 0.1754 mL 0.3507 mL 0.8768 mL
100 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7014 mL
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DCZ0415 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DCZ04152242470-43-3DCZ 0415DCZ-0415NF-κBApoptosisNuclear factor-κBNuclear factor-kappaBTRIP13nonhomologousendjoiningrepairanti-myelomadrug-resistantmyelomaInhibitorinhibitorinhibit

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