TrimTAC1
Based on 1 Customer Validation
TrimTAC1 is a TRIM21-based PROTAC degrader targeting BRD4, with a DC50 of 0.649 nM. TrimTAC1 selectively degrades multimeric proteins, including those localized in biomolecular condensates, while exerting no effect on monomeric proteins in the dilute phase. This degradation effect can be blocked by Bortezomib (HY-10227) or TAK-243 (HY-100487). TrimTAC1 can be used in research related to pancreatic cancer and autoimmune diseases.
(Pink: BRD4 ligand (HY-13030); Blue: TRIM21 ligand (HY-169356); Black: linker (HY-W088456)).
For research use only. We do not sell to patients.
- Purity: 99.10%
- CAS No.: 3095569-91-5
- Formula: C43H47ClN8O2S2
- Molecular Weight:807.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
BRD4 0.649 nM (DC50) |
In Vitro
TrimTAC1 (24 h) potently degrades BRD4 in PANC-1 cells, with a DC50 of 0.649 nM and a maximum degradation rate of 71%[1].
TrimTAC1 (3 days) inhibits the proliferation of PANC-1 cells, with a GI50 value of 0.103 μM[1].
TrimTAC1 forms a highly stable, low-energy conformation with BRD4. The spatial orientation of this conformation facilitates efficient ubiquitination, which correlates with its experimentally observed high activity in degrading BRD4 within the TRIM21-TrimTAC1-BRD4 ternary complex[1].
TrimTAC1 exhibits high thermodynamic stability and shows strong positive cooperative binding between TRIM21 and BRD4. The interactions in the TRIM21-TrimTAC1-BRD4 ternary complex are mediated by key hydrophobic and electrostatic residues[1].
TrimTAC1 exhibits physicochemical properties consistent with the favorable membrane permeability and solubility required for targeted protein degrader applications (log P = 4.7, log D7.4 = 4.9)[1].
TrimTAC1 (0-20 μM; 12 h) exhibits no molecular glue degrader activity against nucleoporins in IFNγ-pretreated A549 cells[2].
TrimTAC1 (4 h) does not degrade monomeric mEGFP-BRD4BD2 in A549 cells expressing TRIM21D355A[2].
TrimTAC1 (2 μM; 4 h) efficiently degrades condensate-forming NUP98FG-mEGFP-BRD4BD2 in A549 cells expressing TRIM21D355A via a proteasome- and ubiquitination-dependent mechanism[2].
TrimTAC1 (2 μM; 4 h) selectively degrades mEGFP fusion proteins that form condensates (PML, coilin, NPM1) in A549 cells expressing TRIM21D355A, but does not degrade non-condensate-forming mEGFP fusion proteins (CDK4, BTK)[2].
TrimTAC1 (2 μM; 6 h) selectively degrades DNA-induced BRD4BD2-mEGFP-cGAS condensates in HaCaT cells expressing TRIM21D355A, without affecting soluble BRD4BD2-mEGFP-cGAS[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:0, 5 and 20 μM
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Incubation Time:12 h
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Result:No degradation of nuclear pore proteins was observed in IFNγ-pretreated A549 cells treated with the compound, as determined by immunoblotting for the indicated nuclear pore proteins and β-actin.
Chemical Information
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CAS No. 3095569-91-5
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Appearance Solid
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Molecular Weight 807.47
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Formula C43H47ClN8O2S2
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Color Light yellow to yellow
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SMILES
O=C(NCCCN1CCN(CCCN2C(C=CC=C3)=C3SC4=C2C=C(C(C)=O)C=C4)CC1)C[C@H]5C6=NN=C(N6C7=C(C(C8=CC=C(C=C8)Cl)=N5)C(C)=C(S7)C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (123.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.10 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.10 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 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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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Zhang L, et al. TRIM21-Driven Degradation of BRD4: Development of Heterobifunctional Degraders and Investigation of Recruitment and Selectivity Mechanisms. Journal of chemical information and modeling. 2025 Jul 28;65(14):7584-7604. [Content Brief]
[2]. Lu P, et al. Selective degradation of multimeric proteins by TRIM21-based molecular glue and PROTAC degraders. Cell. 2024 Dec 12;187(25):7126-7142.e20. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.2384 mL | 6.1922 mL | 12.3844 mL | 30.9609 mL |
| 5 mM | 0.2477 mL | 1.2384 mL | 2.4769 mL | 6.1922 mL | |
| 10 mM | 0.1238 mL | 0.6192 mL | 1.2384 mL | 3.0961 mL | |
| 15 mM | 0.0826 mL | 0.4128 mL | 0.8256 mL | 2.0641 mL | |
| 20 mM | 0.0619 mL | 0.3096 mL | 0.6192 mL | 1.5480 mL | |
| 25 mM | 0.0495 mL | 0.2477 mL | 0.4954 mL | 1.2384 mL | |
| 30 mM | 0.0413 mL | 0.2064 mL | 0.4128 mL | 1.0320 mL | |
| 40 mM | 0.0310 mL | 0.1548 mL | 0.3096 mL | 0.7740 mL | |
| 50 mM | 0.0248 mL | 0.1238 mL | 0.2477 mL | 0.6192 mL | |
| 60 mM | 0.0206 mL | 0.1032 mL | 0.2064 mL | 0.5160 mL | |
| 80 mM | 0.0155 mL | 0.0774 mL | 0.1548 mL | 0.3870 mL | |
| 100 mM | 0.0124 mL | 0.0619 mL | 0.1238 mL | 0.3096 mL |
TrimTAC1 Related Classifications
HY-169355 Related Classifications
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