BRD4 degrader AT1
Based on 2 publication(s) in Google Scholar
BRD4 degrader AT1 is a selective PROTAC BRD4 degrader. BRD4 degrader AT1 induces depletion of Brd4 protein in cells. BRD4 degrader AT1 exhibits highly selective depletion of Brd4 over Brd2 and Brd3 in cells.
(Pink: BRD4 ligand (HY-13030); Blue: VHL ligand (HY-111823); Black: linker).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.68%
- CAS No.: 2098836-45-2
- 화학식: C48H58ClN9O5S3
- 분자량:972.68
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) BRD4 degrader AT1
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Biological Activity
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BRD4 |
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Cell Line
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Type | Value | Description | References |
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| HeLa | DC50 |
>=10 nM
Compound: 10; AT1
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Protac activity at VHL/BRD4 short isoform in human HeLa cells assessed as induction of BRD4 short isoform degradation incubated for 24 hrs by Western blot analysis
Protac activity at VHL/BRD4 short isoform in human HeLa cells assessed as induction of BRD4 short isoform degradation incubated for 24 hrs by Western blot analysis
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[PMID: 31047748] |
BRD4 degrader AT1 drives the formation of a positively cooperative ternary complex with VCB and BET bromodomains, among which the Brd4BD2:AT1:VCB complex exhibits the highest cooperativity and stability[1].
BRD4 degrader AT1 (0.01-3 μM; 24 h) potently and selectively depletes Brd4 protein, with no significant effect on the levels of Brd2 or Brd3[1].
BRD4 degrader AT1 (24 h) selectively depletes Brd4 levels to approximately 40% of the baseline in HeLa cells, with no significant effects on Brd2, Brd3, or the vast majority of other detected cellular proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human HeLa cells
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Concentration:0.01, 0.03, 0.1, 0.3, 1, 3 μM
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Incubation Time:24 h
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Result:Induced marked depletion of Brd4 at both 1 μM and 3 μM concentrations after 24 hours.
Showed negligible activity against Brd2 and Brd3.
Chemical Information
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CAS No. 2098836-45-2
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Appearance Solid
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분자량 972.68
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화학식 C48H58ClN9O5S3
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Color Off-white to light yellow
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SMILES
CC1=C(C)SC2=C1C(C3=CC=C(Cl)C=C3)=N[C@@H](CC(NCCCCCCSC(C)(C)[C@H](NC(C)=O)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)C7=NN=C(C)N27
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Philos Trans R Soc Lond B Biol Sci
2025 Jan 23;380(1918):20230342. PMID: 39842482 -
Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
용액&용해도
DMSO : 100 mg/mL (102.81 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)
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: ≥ 1.17 mg/mL (1.20 mM); Clear solution
This protocol yields a clear solution of ≥ 1.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.7 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: ≥ 1.17 mg/mL (1.20 mM); Clear solution
This protocol yields a clear solution of ≥ 1.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.7 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.
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.
순도&문서
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Data Sheet (272 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
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, 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0281 mL | 5.1404 mL | 10.2809 mL | 25.7022 mL |
| 5 mM | 0.2056 mL | 1.0281 mL | 2.0562 mL | 5.1404 mL | |
| 10 mM | 0.1028 mL | 0.5140 mL | 1.0281 mL | 2.5702 mL | |
| 15 mM | 0.0685 mL | 0.3427 mL | 0.6854 mL | 1.7135 mL | |
| 20 mM | 0.0514 mL | 0.2570 mL | 0.5140 mL | 1.2851 mL | |
| 25 mM | 0.0411 mL | 0.2056 mL | 0.4112 mL | 1.0281 mL | |
| 30 mM | 0.0343 mL | 0.1713 mL | 0.3427 mL | 0.8567 mL | |
| 40 mM | 0.0257 mL | 0.1285 mL | 0.2570 mL | 0.6426 mL | |
| 50 mM | 0.0206 mL | 0.1028 mL | 0.2056 mL | 0.5140 mL | |
| 60 mM | 0.0171 mL | 0.0857 mL | 0.1713 mL | 0.4284 mL | |
| 80 mM | 0.0129 mL | 0.0643 mL | 0.1285 mL | 0.3213 mL | |
| 100 mM | 0.0103 mL | 0.0514 mL | 0.1028 mL | 0.2570 mL |
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