| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
TZ9 targets the Rad6B ubiquitin-conjugating enzyme (E2 enzyme). It is a selective and cell-permeable inhibitor that binds to the catalytic site of Rad6B, preventing the ubiquitination of its substrates. This inhibition disrupts the ubiquitin-proteasome pathway, which is critical for regulating protein degradation and various cellular functions. The compound's selectivity for Rad6B makes it a valuable tool for studying the specific role of this E2 enzyme.
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| ln Vitro |
Rad6B SMI #9, TZ9 (0.5-100 µM; 72 hours) inhibits the migration and proliferation of MDA-MB-231 cells [1]. In MDA-MB-231 cells, TZ9 (0.1–5 µM; 24-72 hours) postpones the advancement of the cell cycle [1]. MDA-MB-231 cells undergo apoptosis when exposed to TZ9 (5 µM; 8–48 hours) [1]. In MDA-MB-231 cells, TZ9 (0.5, 1, 2.5, and 5 µM; 24 hours) suppresses H2A ubiquitination and lowers the levels of PCNA and β-catenin protein [1].
In vitro, TZ9 has been shown to be a potent inhibitor of Rad6B activity. It inhibits Rad6B-induced histone H2A ubiquitination and downregulates intracellular β-catenin. The compound inhibits the proliferation of MDA-MB-231 breast cancer cells with an IC50 of approximately 6 µM. At concentrations of 10 µM or higher, it induces morphological changes in cells. |
| ln Vivo |
In vivo, TZ9 is being evaluated for its anti-cancer activity. As an inhibitor of Rad6B, it is expected to disrupt protein degradation pathways that are critical for cancer cell survival. Its effects on tumor growth are being studied in preclinical models.
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| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for TZ9 involve measuring its direct inhibition of Rad6B enzymatic activity. The assay uses a purified recombinant Rad6B enzyme and a substrate (ubiquitin and a target protein). The ubiquitination of the substrate is measured using a radioactive or fluorescent method. The compound is incubated with the enzyme and substrate, and the decrease in ubiquitination is measured to determine the IC50.
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| Cell Assay |
Cell proliferation assay [1]
Cell Types: MDA-MB-231 Cell Tested Concentrations: 0.5-100 µM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibits MDA-MB-231 cell proliferation, IC50 ~6µM. Apoptosis analysis[1] Cell Types: MDA-MB-231 Cell Tested Concentrations: 5 µM Incubation Duration: 8-48 hrs (hours) Experimental Results: Induction of apoptosis. Cell cycle analysis[1] Cell Types: MDA-MB-231 Cell Tested Concentrations: 0.1-5 µM Incubation Duration: 24-72 hrs (hours) Experimental Results: 2-fold increase in the proportion of G2-M arrested cells, accompanied by a proportional increase at 24 hrs (hours) diminished cells in S phase. Dramatically increased percentage of cells stained for cytoplasmic/nuclear cyclin B1. Western Blot Analysis [1] Cell Types: MDA-MB-231 Cell Tested Concentrations: 0.5, 1, 2.5, 5 µM Incubation Duration: 24 h Experimental Results: Inhibited H2A ubiquitination and diminished PCNA and β-catenin protein levels. In vitro cell-based assays for TZ9 are performed using cancer cell lines, such as MDA-MB-231 breast cancer cells. Cells are treated with the compound, and cell viability and proliferation are assessed using standard assays. The compound's effects on histone H2A ubiquitination and β-catenin levels are analyzed by Western blotting. |
| Animal Protocol |
In vivo animal experiments for TZ9 are conducted using mouse xenograft models of cancer. Mice bearing subcutaneous tumors are treated with the compound, and tumor volume is measured over time. The compound's effects on tumor growth and survival are evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of TZ9 have been characterized to support its use as a research tool. The compound has a molecular weight of 366.33 and a formula of C₁₇H₁₄N₆O₄. It is soluble in DMSO. Specific PK parameters, such as half-life and bioavailability, are determined in preclinical studies via LC-MS/MS analysis of plasma samples.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for TZ9 are typical of a research compound. It is generally well-tolerated at effective doses. The safety profile is being evaluated in the context of its use as a research tool to study Rad6B biology.
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| References | |
| Additional Infomation |
Other information: TZ9 is a research compound used to study the role of Rad6B in cancer and other diseases. It is available from chemical suppliers for preclinical research purposes.
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| Molecular Formula |
C17H14N6O4
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|---|---|
| Molecular Weight |
366.33
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| Exact Mass |
366.107
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| CAS # |
1002789-86-7
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| PubChem CID |
7593228
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
675.9±65.0 °C at 760 mmHg
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| Flash Point |
362.6±34.3 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.711
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| LogP |
1.75
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
502
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)NC2=NC(=NC(=N2)N)COC(=O)C3=CC=C(C=C3)[N+](=O)[O-]
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| InChi Key |
RRRDZFQRNJTKHL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H14N6O4/c18-16-20-14(21-17(22-16)19-12-4-2-1-3-5-12)10-27-15(24)11-6-8-13(9-7-11)23(25)26/h1-9H,10H2,(H3,18,19,20,21,22)
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| Chemical Name |
(4-amino-6-anilino-1,3,5-triazin-2-yl)methyl 4-nitrobenzoate
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| Synonyms |
TZ 9; TZ-9; TZ9
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ≥ 40 mg/mL (~109.19 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2730 mL | 1.3649 mL | 2.7298 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.
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