Cat. No.: HY-18643

TZ9

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

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.

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Pureté: 99.27%
CAS No.: 1002789-86-7
Formule: C₁₇H₁₄N₆O₄
Masse moléculaire:366.33

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

TZ9 Chemical Structure

CAS No.: 1002789-86-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- Cellular Effect
- In Vitro
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	7.8 μM Compound: TZ9	Cytotoxicity against human A2780 cells after 72 hrs by MTS assay Cytotoxicity against human A2780 cells after 72 hrs by MTS assay	[PMID: 26965855]
A549	IC₅₀	7.2 μM Compound: TZ9	Cytotoxicity against human A549 cells after 72 hrs by MTS assay Cytotoxicity against human A549 cells after 72 hrs by MTS assay	[PMID: 26965855]
HT-29	IC₅₀	8.3 μM Compound: TZ9	Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay	[PMID: 26965855]
MCF7	IC₅₀	5 μM Compound: TZ9	Cytotoxicity against human MCF7 cells after 72 hrs by MTS assay Cytotoxicity against human MCF7 cells after 72 hrs by MTS assay	[PMID: 26965855]
MDA-MB-231	GI₅₀	10 μM Compound: 20	Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 27362876]
MDA-MB-231	IC₅₀	4.6 μM Compound: SMI#9	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 35981459]
MDA-MB-231	IC₅₀	4.6 μM Compound: TZ9	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTS assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTS assay	[PMID: 26965855]
MDA-MB-231	IC₅₀	6 μM Compound: 67	Inhibition of cell survival in human MDA-MB-231 cells incubated for 72 hrs by MTT assay Inhibition of cell survival in human MDA-MB-231 cells incubated for 72 hrs by MTT assay	[PMID: 39018924]
NCI-H1299	IC₅₀	45 μM Compound: TZ9	Cytotoxicity against human H1299 cells after 72 hrs by MTS assay Cytotoxicity against human H1299 cells after 72 hrs by MTS assay	[PMID: 26965855]
OV-90	IC₅₀	60 μM Compound: TZ9	Cytotoxicity against human OV90 cells after 72 hrs by MTS assay Cytotoxicity against human OV90 cells after 72 hrs by MTS assay	[PMID: 26965855]

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.

Chemical Information

CAS No. 1002789-86-7
Appearance Solid
Masse moléculaire 366.33
Formule C₁₇H₁₄N₆O₄
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Journal Impact Factor

Int J Mol Sci

A Machine Learning Model to Predict Survival and Therapeutic Responses in Multiple Myeloma. [Abstract]

2023 Apr 3;24(7):6683. PMID: 37047654
Biochem Bioph Res Co

Loss of RAD6B induces degeneration of the cochlea in mice. [Abstract]

2020 Oct 20;531(3):402-408. PMID: 32868078

Solvant et solubilité

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7298 mL

13.6489 mL

27.2978 mL

5 mM

0.5460 mL

2.7298 mL

5.4596 mL

10 mM

0.2730 mL

1.3649 mL

2.7298 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Sanders MA, et al. Novel inhibitors of Rad6 ubiquitin conjugating enzyme: design, synthesis, identification, and functional characterization. Mol Cancer Ther. 2013 Apr;12(4):373-83. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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TZ9

Apoptosis Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Ubiquitination Compound Library

Anti-Breast Cancer Compound Library

Anti-Liver Cancer Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) TZ9

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

TZ9

Apoptosis Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Ubiquitination Compound Library

Anti-Breast Cancer Compound Library

Anti-Liver Cancer Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) TZ9

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

TZ9 Related Classifications

HY-18643 Related Classifications