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, BRD4Short and BRD4Long 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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- Formule: C74H91ClFN11O17S2
- Masse moléculaire:1525.16
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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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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Cell Line
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Type | Value | Description | References |
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| HEK293 | DC50 |
2.3 nM
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Degradation of BRD4Long protein in HEK293 cells measured via Western blot after 6 hours of incubation.
Degradation of BRD4Long protein in HEK293 cells measured via Western blot after 6 hours of incubation.
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39606859 |
| HEK293 | DC50 |
2.1 nM
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Degradation of BRD4Short protein in HEK293 cells measured via Western blot after 6 hours of incubation.
Degradation of BRD4Short protein in HEK293 cells measured via Western blot after 6 hours of incubation.
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39606859 |
| HEK293 | DC50 |
1.6 nM
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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.
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39606859 |
| HEK293 | DC50 |
15 nM
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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.
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39606859 |
| HEK293 | DC50 |
75 nM
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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.
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39606859 |
| RKO | EC50 |
111 nM
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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.
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39606859 |
| RKO | EC50 |
133 nM
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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.
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39606859 |
| RKO | EC50 |
180 nM
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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.
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39606859 |
| RKO | EC50 |
988 nM
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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.
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39606859 |
| HEK293 | IC50 |
2282 nM
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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.
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39606859 |
| HEK293 | IC50 |
624 nM
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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.
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39606859 |
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 BRD4Long, BRD4Short, 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.
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Cell Line:HEK293 cells
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Concentration:0.1, 1, 10, 100, 1000 nM
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Incubation Time:6 h
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Result:Degraded BRD4Long, BRD4Short, 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
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Masse moléculaire 1525.16
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Formule C74H91ClFN11O17S2
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AB3067 Related Classifications
HY-170390 Related Classifications
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