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Art. -Nr.: HY-170390

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AB3067

AB3067 is a PROTAC degrader of BET that simultaneously recruits the E3 ligase activities of CRBN and VHL. The DC₅₀ values of AB3067 against BRD2, BRD3, BRD4^Short and BRD4^Long are 15 nM, 1.6 nM, 2.1 nM and 2.3 nM, respectively. AB3067 induces additive protein ubiquitination and proteasomal degradation, and minimizes the cross-degradation of E3 ligases. AB3067 can be used in colon cancer-related studies.
(Pink: BET ligand (HY-131633A) and no Target protein ligand; Blue: Cereblon ligand (HY-W998346) and VHL ligand (HY-112078); Black: linker and linker).

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Formel: C₇₄H₉₁ClFN₁₁O₁₇S₂
Molecular Weight:1525.16

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

AB3067 Chemical Structure

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Preis

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

AB3067 is a PROTAC degrader of BET that simultaneously recruits the E3 ligase activities of CRBN and VHL. The DC₅₀ values of AB3067 against BRD2, BRD3, BRD4^Short and BRD4^Long are 15 nM, 1.6 nM, 2.1 nM and 2.3 nM, respectively. AB3067 induces additive protein ubiquitination and proteasomal degradation, and minimizes the cross-degradation of E3 ligases. AB3067 can be used in colon cancer-related studies^[1]^[2]^[3]. (Pink: BET ligand (HY-131633A) and no Target protein ligand; Blue: Cereblon ligand (HY-W998346) and VHL ligand (HY-112078); Black: linker and linker).

IC₅₀ & Target^[1]

BRD2

15 nM (DC₅₀)

BRD3

1.6 nM (DC₅₀)

BRD4

2.1 nM (DC₅₀, short)

BRD4

2.3 nM (DC₅₀, long)

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Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	DC₅₀	2.3 nM	Degradation of BRD4^Long protein in HEK293 cells measured via Western blot after 6 hours of incubation. Degradation of BRD4^Long protein in HEK293 cells measured via Western blot after 6 hours of incubation.	39606859
HEK293	DC₅₀	2.1 nM	Degradation of BRD4^Short protein in HEK293 cells measured via Western blot after 6 hours of incubation. Degradation of BRD4^Short protein in HEK293 cells measured via Western blot after 6 hours of incubation.	39606859
HEK293	DC₅₀	1.6 nM	Degradation of BRD3 protein in HEK293 cells measured via Western blot after 6 hours of incubation. Degradation of BRD3 protein in HEK293 cells measured via Western blot after 6 hours of incubation.	39606859
HEK293	DC₅₀	15 nM	Degradation of BRD2 protein in HEK293 cells measured via Western blot after 6 hours of incubation. Degradation of BRD2 protein in HEK293 cells measured via Western blot after 6 hours of incubation.	39606859
HEK293	DC₅₀	75 nM	Degradation of CRBN protein in HEK293 cells measured via Western blot after 6 hours of incubation. Degradation of CRBN protein in HEK293 cells measured via Western blot after 6 hours of incubation.	39606859
RKO	EC₅₀	111 nM	Antiproliferative activity against wild-type RKO colon carcinoma cells measured via normalized cell viability assay. Antiproliferative activity against wild-type RKO colon carcinoma cells measured via normalized cell viability assay.	39606859
RKO	EC₅₀	133 nM	Antiproliferative activity against CRBN knockout RKO colon carcinoma cells measured via normalized cell viability assay. Antiproliferative activity against CRBN knockout RKO colon carcinoma cells measured via normalized cell viability assay.	39606859
RKO	EC₅₀	180 nM	Antiproliferative activity against VHL knockout RKO colon carcinoma cells measured via normalized cell viability assay. Antiproliferative activity against VHL knockout RKO colon carcinoma cells measured via normalized cell viability assay.	39606859
RKO	EC₅₀	988 nM	Antiproliferative activity against CRBN/VHL double knockout RKO colon carcinoma cells measured via normalized cell viability assay. Antiproliferative activity against CRBN/VHL double knockout RKO colon carcinoma cells measured via normalized cell viability assay.	39606859
HEK293	IC₅₀	2282 nM	Engagement of VHL in HEK293 cells measured via live cell NanoBRET target engagement assay with competitive displacement of fluorescent tracer after 2 hours of incubation. Engagement of VHL in HEK293 cells measured via live cell NanoBRET target engagement assay with competitive displacement of fluorescent tracer after 2 hours of incubation.	39606859
HEK293	IC₅₀	624 nM	Engagement of CRBN in HEK293 cells measured via live cell NanoBRET target engagement assay with competitive displacement of fluorescent tracer after 2 hours of incubation. Engagement of CRBN in HEK293 cells measured via live cell NanoBRET target engagement assay with competitive displacement of fluorescent tracer after 2 hours of incubation.	39606859

In Vitro

AB3067 (compound 27) (1 nM-10 μM) induces potent antiproliferative effects in BET-sensitive RKO cells, and shows reduced activity only in the dual ligase knockout cell line^[1].
AB3067 (100 pM-1 μM; 6 h) potently degrades BRD4^Long, BRD4^Short, BRD3 and BRD2 in HEK293 cells, with DC₅₀ values of 2.3 nM, 2.1 nM, 1.6 nM and 15 nM, respectively^[1].
AB3067 (4 nM-3 μM) potently and rapidly degrades BRD2, BRD3 and BRD4 in HiBiT-tagged HEK293 cells^[1].
AB3067 (0.01-1 μM; 3.5 h) forms a dose-dependent ternary complex with BRD4 and either VHL or CRBN in HiBiT-BRD4 HEK293 cells^[1].
The potent and rapid BRD4-degrading effect of AB3067 (5 pM-3 μM) in HiBiT-BRD4 HEK293 cells depends on the two ligases CRBN and VHL, and the effects of the two ligases are additive^[1].
AB3067 (12 nM-3 μM; 4 h) induces BRD4 ubiquitination in HiBiT-BRD4 HEK293 cells, and both CRBN and VHL contribute to the rate and extent of ubiquitination^[1].
AB3067 (250 nM; 4 h) selectively degrades BRD2, BRD3 and BRD4 in HEK293 cells, with no significant off-target protein degradation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

HEK293 cells
Concentration:

0.1, 1, 10, 100, 1000 nM
Incubation Time:

6 h
Result:

Degraded BRD4^Long, BRD4^Short, BRD3 and BRD2 in HEK293 cells, with DC₅₀ values of 2.3 nM, 2.1 nM, 1.6 nM and 15 nM, respectively

Chemical Information

Molecular Weight 1525.16
Formel C₇₄H₉₁ClFN₁₁O₁₇S₂
SMILES

O=C(OCCOCCOCCOCC(C)(COCCOCCOCCNC1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2=O)=O)C=C1F)COCC(N[C@H](C(N4[C@H](C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)C[C@@H](O)C4)=O)C(C)(C)C)=O)C[C@H]7C8=NN=C(C)N8C9=C(C(C)=C(C)S9)C(C%10=CC=C(Cl)C=C%10)=N7
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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]. Bond AG, et al. Leveraging Dual-Ligase Recruitment to Enhance Protein Degradation via a Heterotrivalent Proteolysis Targeting Chimera. Journal of the American Chemical Society. 2024 Dec 11;146(49):33675-33711. [Content Brief]

[2]. Zhu W, et al. Modular Assembled Targeting Chimera Enables Multimodal Targeted Protein Degradation. JACS Au. 2025 Nov 24;5(11):5635-5647.

[3]. Cao Y, et al. Branching beyond bifunctional linkers: synthesis of macrocyclic and trivalent PROTACs. Nature protocols. 2026 May;21(5):2328-2363.

Calculators

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)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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AB3067

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