ZXH-3-26
Based on 3 publication(s) in Google Scholar
ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC50/5h of 5 nM. The DC50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM.
(Pink: BRD4 ligand (HY-43723); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W012971)).
For research use only. We do not sell to patients.
- Purity: 99.53%
- CAS No.: 2243076-67-5
- Formula: C38H37ClN8O7S
- Molecular Weight:785.27
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Storage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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
Publications Citing Use of MedChemExpress (MCE) ZXH-3-26
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Customer Validation & Images
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WB
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WB
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IF
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IF
All PROTACs Isoforms
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Biological Activity
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BRD4 5 nM (DC50, 5 hours of treatment) |
Cereblon |
ZXH-3-26 represents the first small molecule to allow pharmacologic targeting of BRD4 without significant inhibition or degradation of BRD2/3[1].
ZXH-3-26 shows activity exclusively on the first bromodomain of BRD4, and spares degradation of BRD2/3 at concentrations 10 μM. Immunoblot analysis confirms that ZXH-3-26 degrades endogenous BRD4 with comparable efficacy compared to the best pan-BET degrader dBET6, while being inactive on BRD2/3[1].
ZXH-3-26 engages CRBN in a conformation distinct[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2243076-67-5
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Appearance Solid
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Molecular Weight 785.27
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Formula C38H37ClN8O7S
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Color Light yellow to yellow
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SMILES
O=C(OC)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C(NCCCCCNC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)=O)S3)C(C7=CC=C(Cl)C=C7)=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Discov
2023 May 9;9(1):47. PMID: 37156794
ZXH-3-26 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2023 May 9;9(1):47. [Abstract]
ZXH-3-26 (0.001, 0.005, 0.01, 0.025, 0.05, 0.1, 0.3, 1, 10 μM; 6 h) inhibits the expression of the long (BRD4 l) and the short (BRD4 s) isoform in HeLa cells.
ZXH-3-26 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2023 May 9;9(1):47. [Abstract]
ZXH-3-26 (100 nM; 0.5, 1, 2, 4, 6, 8, 12, 24 h) inhibits the expression of the long (BRD4 l) and the short (BRD4 s) isoform in HeLa cells.
ZXH-3-26 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2023 May 9;9(1):47. [Abstract]
ZXH-3-26 (0.01, 0.05, 0.1, 0.3, 1, 0.3, 10 μM; 6 h) inhibits the expression of the long (BRD4 l) and the short (BRD4 s) isoform in HeLa cells.
ZXH-3-26 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2023 May 9;9(1):47. [Abstract]
ZXH-3-26 (100 nM; 0.5, 2, 4, 6, 12, 24 h) inhibits the expression of the long (BRD4 l) and the short (BRD4 s) isoform in HeLa cells.
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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 -
Solvent & Solubility
DMSO : 50 mg/mL (63.67 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 (stored under nitrogen). 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 (stored under nitrogen). 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: ≥ 5 mg/mL (6.37 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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 (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 (stored under nitrogen). 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 | 1.2734 mL | 6.3672 mL | 12.7345 mL | 31.8362 mL |
| 5 mM | 0.2547 mL | 1.2734 mL | 2.5469 mL | 6.3672 mL | |
| 10 mM | 0.1273 mL | 0.6367 mL | 1.2734 mL | 3.1836 mL | |
| 15 mM | 0.0849 mL | 0.4245 mL | 0.8490 mL | 2.1224 mL | |
| 20 mM | 0.0637 mL | 0.3184 mL | 0.6367 mL | 1.5918 mL | |
| 25 mM | 0.0509 mL | 0.2547 mL | 0.5094 mL | 1.2734 mL | |
| 30 mM | 0.0424 mL | 0.2122 mL | 0.4245 mL | 1.0612 mL | |
| 40 mM | 0.0318 mL | 0.1592 mL | 0.3184 mL | 0.7959 mL | |
| 50 mM | 0.0255 mL | 0.1273 mL | 0.2547 mL | 0.6367 mL | |
| 60 mM | 0.0212 mL | 0.1061 mL | 0.2122 mL | 0.5306 mL |
ZXH-3-26 Related Classifications
HY-122826 Related Classifications
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