KB02-JQ1
Based on 4 publication(s) in Google Scholar
KB02-JQ1 is a potent and selective BRD4 PROTAC degrader. KB02-JQ1 degrades BRD4 via the ubiquitin-proteasome pathway by bridging DCAF16 E3 ubiquitin ligase and BRD4. KB02-JQ1 can be used for cancer research.
(Pink: BRD4 ligand (HY-78695); Blue: DCAF16 ligand (HY-131385); Black: linker (HY-128833)).
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
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Biological Activity
Description
IC50 & Target
[1]|
BRD4 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
>50 μM
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Cytotoxicity against human HEK293T cells.
Cytotoxicity against human HEK293T cells.
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31209349 |
In Vitro
KB02-JQ1 (4-40 μM) induces concentration-dependent proteasomal degradation of endogenous BRD4 in HEK293T cells, whereas KB02 alone, JQ1 alone, and their combination do not exhibit this effect[1].
KB02-JQ1 (20 μM; 2 h) promotes the formation of a complex between BRD4 and high-molecular-weight covalently modified HA-DCAF16 in HEK293T cells co-transfected with BRD4-FLAG and HA-DCAF16[1].
KB02-JQ1 (40 μM; 24 h) induces BRD4 degradation in DCAF16+/+ HEK293 cells, but this effect is significantly blocked in DCAF16-/- cells, indicating that its degradation effect is dependent on DCAF16[1].
KB02-JQ1 (incubation for 24 h) has minimal effect on HEK293T cell viability, with an IC50 > 50 μM[1].
KB02-JQ1 (20 μM; 1.5 h) produces approximately 40% covalent binding with DCAF16 (C173/177-179 peptide) in HEK293T cells[1].
KB02-JQ1 (20 μM; 24 h) selectively decreases BRD4 and ACAT1 protein abundance and stabilizes BRD2 protein abundance in SILAC-labeled 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, 10, 20, 40 μM
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Incubation Time:24 h
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Result:Induced the degradation of endogenous BRD4 in a concentration-dependent manner.
Effectively degraded BRD4, whereas the monomeric components and their uncoupled combination failed to induce degradation.
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Cell Line:HEK293 DCAF16+/+ and DCAF16-/- cells
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Concentration:40 μM
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Incubation Time:24 h
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Result:Substantially degraded BRD4 in DCAF16+/+ cells, but the degradation was heavily blocked in DCAF16 knockout 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
In Vitro:
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)
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 (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.
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 (282 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 |
|---|---|---|---|---|---|
| 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 |
KB02-JQ1 Related Classifications
HY-129917 Related Classifications
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