| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
TMX1 targets BRD4, specifically the BD2 domain. It is a molecular glue degrader that selectively recruits DCAF16 to BRD4 BD2, inducing BRD4 degradation. It is a covalent degrader. This mechanism is distinct from traditional PROTACs as it does not require a separate linker.
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| ln Vitro |
In vitro, TMX1 is a potent and selective covalent degrader of BRD4 via DCAF16. It functions as a molecular glue to recruit DCAF16 selectively to BRD4 BD2, causing degradation of BRD4. Its selectivity for BRD4 over other bromodomain-containing proteins is a key feature.
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| ln Vivo |
Specific in vivo activity data for TMX1 are not detailed in the search results.
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| Enzyme Assay |
Non-cellular assays for TMX1 are not typically performed, as it is a degrader that functions in a cellular context by hijacking the ubiquitin-proteasome system. Its activity is assessed by measuring the degradation of the BRD4 protein in cells.
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| Cell Assay |
In vitro cellular assays for TMX1 are performed using cells expressing BRD4. Cells are treated with the compound, and the degradation of BRD4 is measured by Western blotting. The selectivity of the degrader for BRD4 over other proteins can also be assessed.
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| Animal Protocol |
In vivo animal experiments for TMX1 would typically be conducted in mouse xenograft models using cancer cell lines dependent on BRD4. The compound would be administered via intraperitoneal or oral routes, and tumor growth inhibition and BRD4 degradation in tumor tissues would be assessed.
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| ADME/Pharmacokinetics |
TMX1 has a molecular weight of 476.59. Its CAS number is 3079093-92-5. It is a molecular glue degrader. Its molecular formula is C26H28N4O3S.
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| Toxicity/Toxicokinetics |
Toxicological data for TMX1 are not detailed in the search results. As a degrader of BRD4, a protein involved in transcriptional regulation, its toxicity profile would depend on its selectivity and the importance of BRD4 in normal cells.
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| References | |
| Additional Infomation |
TMX1 is a molecular glue degrader targeting BRD4. It selectively recruits DCAF16 to the BRD4 BD2 domain, leading to degradation of BRD4. It is a research compound used to study the role of BRD4 in cancer and other diseases.
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| Molecular Formula |
C26H28N4O3S
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|---|---|
| Molecular Weight |
476.59
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| Appearance |
White to off-white solid powder
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 :≥ 100 mg/mL (~209.82 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.25 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: ≥ 2.5 mg/mL (5.25 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0982 mL | 10.4912 mL | 20.9824 mL | |
| 5 mM | 0.4196 mL | 2.0982 mL | 4.1965 mL | |
| 10 mM | 0.2098 mL | 1.0491 mL | 2.0982 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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