KB02-JQ1
Based on 4 publication(s) in Google Scholar
KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1.
For research use only. We do not sell to patients.
- Purity: 99.10%
- CAS No.: 2384184-44-3
- Formula: C38H43Cl2N7O6S
- Molecular Weight:796.76
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Storage:Powder -20°C, 3 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
Publications Citing Use of MedChemExpress (MCE) KB02-JQ1
MoreAll PROTACs Isoforms
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Biological Activity
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BRD4 |
KB02-JQ1 (5-40 μM; 24 hours; HEK293T cells) treatment shows concentration-dependent degradation of endogenous BRD4 in HEK293T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells
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Concentration:5 μM, 10 μM, 20 Μm or 40 μM
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Incubation Time:24 hours
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Result:Concentration-dependent degradation of endogenous BRD4 in HEK293T cells.
Chemical Information
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CAS No. 2384184-44-3
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Appearance Solid
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Molecular Weight 796.76
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Formula C38H43Cl2N7O6S
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Color White to off-white
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SMILES
O=C(NCCOCCOCCNC(C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1)=O)COC5=CC6=C(N(C(CCl)=O)CCC6)C=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Chem Biol
2024 Dec;20(12):1640-1649. PMID: 39075252 -
Elife
2024 Sep 4:13:RP93256. PMID: 39230574 -
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bioRxiv
Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders. [Abstract]2023 Feb 15:2023.02.14.528208. PMID: 36824856
Solvent & Solubility
DMSO : 100 mg/mL (125.51 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: ≥ 5 mg/mL (6.28 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (6.28 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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 (281 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
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 | 1.2551 mL | 6.2754 mL | 12.5508 mL | 31.3771 mL |
| 5 mM | 0.2510 mL | 1.2551 mL | 2.5102 mL | 6.2754 mL | |
| 10 mM | 0.1255 mL | 0.6275 mL | 1.2551 mL | 3.1377 mL | |
| 15 mM | 0.0837 mL | 0.4184 mL | 0.8367 mL | 2.0918 mL | |
| 20 mM | 0.0628 mL | 0.3138 mL | 0.6275 mL | 1.5689 mL | |
| 25 mM | 0.0502 mL | 0.2510 mL | 0.5020 mL | 1.2551 mL | |
| 30 mM | 0.0418 mL | 0.2092 mL | 0.4184 mL | 1.0459 mL | |
| 40 mM | 0.0314 mL | 0.1569 mL | 0.3138 mL | 0.7844 mL | |
| 50 mM | 0.0251 mL | 0.1255 mL | 0.2510 mL | 0.6275 mL | |
| 60 mM | 0.0209 mL | 0.1046 mL | 0.2092 mL | 0.5230 mL | |
| 80 mM | 0.0157 mL | 0.0784 mL | 0.1569 mL | 0.3922 mL | |
| 100 mM | 0.0126 mL | 0.0628 mL | 0.1255 mL | 0.3138 mL |
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