Art. -Nr.: HY-129917

KB02-JQ1

Name: KB02-JQ1
Brand: MedChemExpress
SKU: HY-129917
Price: 380.00 USD
Availability: InStock
Rating: 5 (4 reviews)

4 Cited Publications

Kundenbewertung

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)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.10%
CAS. Nr.: 2384184-44-3
Formel: C₃₈H₄₃Cl₂N₇O₆S
Molecular Weight:796.76

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

KB02-JQ1 Chemical Structure

CAS. Nr.: 2384184-44-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]. (Pink: BRD4 ligand (HY-78695); Blue: DCAF16 ligand (HY-131385); Black: linker (HY-128833)).

IC₅₀ & Target

^[1]

BRD4

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	IC₅₀	>50 μM	Cytotoxicity against human HEK293T cells. Cytotoxicity against human HEK293T cells.	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.

Western Blot Analysis^[1]

Cell Line:

HEK293T cells
Concentration:

5, 10, 20, 40 μM
Incubation Time:

24 h
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.

Western Blot Analysis^[1]

Cell Line:

HEK293 DCAF16+/+ and DCAF16-/- cells
Concentration:

40 μM
Incubation Time:

24 h
Result:

Substantially degraded BRD4 in DCAF16+/+ cells, but the degradation was heavily blocked in DCAF16 knockout cells.

Chemical Information

CAS. Nr. 2384184-44-3
Appearance Solid
Molecular Weight 796.76
Formel C₃₈H₄₃Cl₂N₇O₆S
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (4)

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Journal Impact Factor

Nat Chem Biol

Template-assisted covalent modification underlies activity of covalent molecular glues. [Abstract]

2024 Dec;20(12):1640-1649. PMID: 39075252
Elife

Quantitative mapping of proteasome interactomes and substrates using ProteasomeID. [Abstract]

2024 Sep 4:13:RP93256. PMID: 39230574
Harvard University

2023 Mar. 30487357.
bioRxiv

Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders. [Abstract]

2023 Feb 15:2023.02.14.528208. PMID: 36824856

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2551 mL

6.2754 mL

12.5508 mL

5 mM

0.2510 mL

1.2551 mL

2.5102 mL

10 mM

0.1255 mL

0.6275 mL

1.2551 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (6.28 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhang X, et al. Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16. Nature chemical biology. 2019 Jul;15(7):737-746. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

KB02-JQ1

4 Cited Publications

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KB02-JQ1

Publications Citing Use of MedChemExpress (MCE) KB02-JQ1

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen