JQ1-JX5
Based on 1 Customer Validation
JQ1-JX5 is a DCAF16-based BRD4 PROTAC degrader. JQ1-JX5 covalently modifies Cys58 of DCAF16, promotes ternary complex formation with BRD4, enables BRD4 ubiquitination and proteasomal degradation. JQ1-JX5 induces time-dependent degradation of BRD4 long and short isoforms in AGS cells with DC50 of 43.97 and 16.77 nM. JQ1-JX5 can be used for the research of cancer, such as acute myeloid leukemia.
(Pink: BRD4 ligand (HY-78695); Blue: DCAF16 ligand (HY-W005799); Black: linker).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.69%
- Formel: C29H24ClN7O2S2
- Molecular Weight:602.13
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
BRD4 |
DCAF16 |
In Vitro
JQ1-JX5 (1.0 μM; 3-36 h) induces time-dependent degradation of BRD4 long and short isoforms in AGS cells with DC50 of 43.97 and 16.77 nM, and ~90% loss of both isoforms achieved by 24 hours[1].
JQ1-JX5 (0.01-5 μM; 12 h) induces degradation of BRD4 long and short isoforms in AGS, MDA-MB-453, AsPC1, MV-4-11, MDA-MB-231, and HEK293T cells[1].
JQ1-JX5 inhibits AGS cells proliferation with an IC50 of 0.4993 μM[1].
JQ1-JX5 mediates the degradation of BRD4 by covalent recruitment of DCAF16[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:AGS cancer cells
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Concentration:1.0 μM
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Incubation Time:3, 6, 9, 12, 24, 36 h
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Result:Induced time-dependent degradation of BRD4, with detectable reduction in both long and short isoforms within 3 h.
Caused ~90% loss of both BRD4 isoforms after 24 h of treatment.
Led to near-complete depletion of both BRD4 isoforms after 36 h.
Chemical Information
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Appearance Solid
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Molecular Weight 602.13
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Formel C29H24ClN7O2S2
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Color White to off-white
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SMILES
CC1=NN=C2[C@@H](N=C(C3=C(N21)SC(C)=C3C)C4=CC=C(C=C4)Cl)CC(NCCOC5=CC=C6N=C(SC6=C5)C#N)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (166.08 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 5 mg/mL (8.30 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.
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.
Reinheit & Dokumentation
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Data Sheet (273 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)
Verweise
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 | 1.6608 mL | 8.3039 mL | 16.6077 mL | 41.5193 mL |
| 5 mM | 0.3322 mL | 1.6608 mL | 3.3215 mL | 8.3039 mL | |
| 10 mM | 0.1661 mL | 0.8304 mL | 1.6608 mL | 4.1519 mL | |
| 15 mM | 0.1107 mL | 0.5536 mL | 1.1072 mL | 2.7680 mL | |
| 20 mM | 0.0830 mL | 0.4152 mL | 0.8304 mL | 2.0760 mL | |
| 25 mM | 0.0664 mL | 0.3322 mL | 0.6643 mL | 1.6608 mL | |
| 30 mM | 0.0554 mL | 0.2768 mL | 0.5536 mL | 1.3840 mL | |
| 40 mM | 0.0415 mL | 0.2076 mL | 0.4152 mL | 1.0380 mL | |
| 50 mM | 0.0332 mL | 0.1661 mL | 0.3322 mL | 0.8304 mL | |
| 60 mM | 0.0277 mL | 0.1384 mL | 0.2768 mL | 0.6920 mL | |
| 80 mM | 0.0208 mL | 0.1038 mL | 0.2076 mL | 0.5190 mL | |
| 100 mM | 0.0166 mL | 0.0830 mL | 0.1661 mL | 0.4152 mL |
JQ1-JX5 Related Classifications
HY-183575 Related Classifications
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