RAJQ14
RAJQ14 is a BRD4 PROTAC-like CAP-TAC (Proteasome Cap Targeting Chimeras) degrader. RAJQ14 binds to 19S proteasome cap subunits RPN1, RPN10, RPN13, and USP14 to recruit target proteins to the proteasome for ubiquitination-independent, proteasome-dependent degradation. RAJQ14 can be used for the research of cancer (Pink: BRD4 Ligand (HY-181496); Blue: Proteasome Ligand (HY-128978); Black: Linker).
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- No. CAS: 2375455-53-9
- Fòrmula: C60H64Cl5N9O4S
- Peso molecular:1184.54
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
BRD4 |
BRD2 |
BRD3 |
In Vitro
RAJQ14 (10 μM) selectively binds to the bromodomains of BRD2, BRD3, and BRD4, increasing their thermal stability[1].
RAJQ14 (10 μM; 2 h) binds to both RPN13 and BRD4 in live HEK293T cells[1].
RAJQ14 (0.1-2.5 μM; 2-24 h) induces dose-dependent and time-dependent degradation of BRD4 in HEK293T cells[1].
RAJQ14 (1 μM; 6 h) selectively induces degradation of BRD2, BRD3, and BRD4 in HEK293T cells, with no off-target degradation of other bromodomain-containing proteins[1].
RAJQ14 (0.1-2.5 μM; 24 h) induces BRD4 degradation in CRBN-knockout HEK293T cells that is independent of the E3 ligase CRBN[1].
RAJQ14 (1-100 μM; overnight) binds to multiple 19S proteasome cap subunits (including RPN1, RPN10, RPN13, and USP14) and BET proteins (BRD2, BRD3, BRD4) in HCT116 cells, independent of RPN13 expression[1].
RAJQ14 (0.1-2.5 μM; 24 h) induces BRD4 degradation in RPN13-knockou HCT116 cells independent of RPN13, likely via engagement of alternative 19S proteasome cap subunits[1].
RAJQ14 (0.1-2.5 μM; 24 h) induces BRD4 degradation in T47D-shRPN1-Dox cells that is not fully dependent on RPN1, as compensatory upregulation of RPN13 and RPN11 maintains degrader activity[1].
RAJQ14 (2.5 μM; 6 h) induces BRD4 degradation in HEK293T cells via a ubiquitination-independent mechanism, as BRD4 ubiquitination is not detected during degradation[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:0.1, 0.25, 0.5, 1, 2.5 μM
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Incubation Time:2, 6, 24 h
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Result:Induced dose-dependent degradation of BRD4 after 24 h, with decreasing protein levels observed at increasing concentrations.
Detected degradation as early as 2 h post-treatment, and persisted through 6 h.
Induced degradation of BRD2, BRD3, and BRD4.
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Cell Line:CRBN-knockout HEK293T cells
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Concentration:0.1, 0.25, 0.5, 1, 2.5 μM
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Incubation Time:24 h
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Result:Induced dose-dependent degradation of BRD4 in CRBN-knockout cells, similar to its activity in wild-type HEK293T cells.
Chemical Information
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No. CAS 2375455-53-9
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Peso molecular 1184.54
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Fòrmula C60H64Cl5N9O4S
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SMILES
O=C(NCCCN1CCN(CCCCCCOC2=CC=C(C[C@H](N)C(N3C/C(C(/C(C3)=C\C4=CC=C(Cl)C(Cl)=C4)=O)=C/C5=CC=C(Cl)C(Cl)=C5)=O)C=C2)CC1)C[C@H]6C7=NN=C(C)N7C8=C(C(C)=C(C)S8)C(C9=CC=C(Cl)C=C9)=N6
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RAJQ14 Related Classifications
HY-181495 Related Classifications
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