1. Metabolic Enzyme/Protease Apoptosis
  2. E1/E2/E3 Enzyme Apoptosis
  3. TZ9

TZ9 is a selective Rad6 inhibitor. TZ9 inhibits Rad6B-induced histone H2A ubiquitination, downregulates intracellular β-catenin, induces G2-M arrest and apoptosis, and inhibits the proliferation and migration of metastatic human breast cancer cells.

For research use only. We do not sell to patients.

TZ9 Chemical Structure

TZ9 Chemical Structure

CAS No. : 1002789-86-7

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 110 In-stock
Solution
10 mM * 1 mL in DMSO USD 110 In-stock
Solid
5 mg USD 100 In-stock
10 mg USD 160 In-stock
50 mg USD 560 In-stock
100 mg USD 850 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

TZ9 is a selective Rad6 inhibitor. TZ9 inhibits Rad6B-induced histone H2A ubiquitination, downregulates intracellular β-catenin, induces G2-M arrest and apoptosis, and inhibits the proliferation and migration of metastatic human breast cancer cells[1].

In Vitro

TZ9 (Rad6B SMI #9) (0.5-100 µM; 72 h) inhibits MDA-MB-231 cell proliferation and migration[1].
TZ9 (0.1-5 µM; 24-72 h) delays cell-cycle progression in MDA-MB-231 cells[1].
TZ9 (5 µM; 8-48 h) induces apoptosis in MDA-MB-231 cells[1].
TZ9 (0.5, 1, 2.5, 5 µM; 24 h) inhibits H2A ubiquitination and downregulates levels of PCNA and β-catenin protein in MDA-MB-231 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5-100 µM
Incubation Time: 72 h
Result: Inhibited MDA-MB-231 cell proliferation with IC50 ~6µM.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 5 µM
Incubation Time: 8-48 h
Result: Induced cells apoptosis.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.1-5 µM
Incubation Time: 24-72 h
Result: Increased the proportion of G2-M-arrested cells by 2-fold and was accompanied by a proportional decrease in S-phase cells when at 24 h.
Significantly increased the percentage of cells with cytoplasmic/nuclear cyclin B1 staining.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 1, 2.5, 5 µM
Incubation Time: 24 h
Result: Inhibited H2A ubiquitination, decreased PCNA and β-catenin protein levels.
Molecular Weight

366.33

Formula

C17H14N6O4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(OCC1=NC(N)=NC(NC2=CC=CC=C2)=N1)C3=CC=C([N+]([O-])=O)C=C3

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 : ≥ 40 mg/mL (109.19 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7298 mL 13.6489 mL 27.2978 mL
5 mM 0.5460 mL 2.7298 mL 5.4596 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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Molecular Weight *

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: ≥ 2.5 mg/mL (6.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

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: 99.45%

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 2.7298 mL 13.6489 mL 27.2978 mL 68.2445 mL
5 mM 0.5460 mL 2.7298 mL 5.4596 mL 13.6489 mL
10 mM 0.2730 mL 1.3649 mL 2.7298 mL 6.8244 mL
15 mM 0.1820 mL 0.9099 mL 1.8199 mL 4.5496 mL
20 mM 0.1365 mL 0.6824 mL 1.3649 mL 3.4122 mL
25 mM 0.1092 mL 0.5460 mL 1.0919 mL 2.7298 mL
30 mM 0.0910 mL 0.4550 mL 0.9099 mL 2.2748 mL
40 mM 0.0682 mL 0.3412 mL 0.6824 mL 1.7061 mL
50 mM 0.0546 mL 0.2730 mL 0.5460 mL 1.3649 mL
60 mM 0.0455 mL 0.2275 mL 0.4550 mL 1.1374 mL
80 mM 0.0341 mL 0.1706 mL 0.3412 mL 0.8531 mL
100 mM 0.0273 mL 0.1365 mL 0.2730 mL 0.6824 mL
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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.

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TZ9
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