2. PROTAC Metabolic Enzyme/Protease Epigenetics
  3. Proteasome Cap Targeting Chimeras PROTACs Proteasome Epigenetic Reader Domain
  4. 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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RAJQ14

RAJQ14 構造式

CAS 番号 : 2375455-53-9

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RAJQ14 関連抗体

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製品説明

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[1] (Pink: BRD4 Ligand (HY-181496); Blue: Proteasome Ligand (HY-128978); Black: Linker).

IC50 & Target[1]

BRD4

 

BRD2

 

BRD3

 

体外実験

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.

RAJQ14 関連抗体

Western Blot Analysis[1]

Cell Line: HEK293T cells
Concentration: 0.1, 0.25, 0.5, 1, 2.5 μM
Incubation Time: 2, 6, 24 h
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.

Western Blot Analysis[1]

Cell Line: CRBN-knockout HEK293T cells
Concentration: 0.1, 0.25, 0.5, 1, 2.5 μM
Incubation Time: 24 h
Result: Induced dose-dependent degradation of BRD4 in CRBN-knockout cells, similar to its activity in wild-type HEK293T cells.
分子量

1184.54

分子式

C60H64Cl5N9O4S
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
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RAJQ14 Related Classifications

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Keywords:

RAJQ142375455-53-9RAJQ 14RAJQ-14Proteasome Cap Targeting ChimerasPROTACsProteasomeEpigenetic Reader DomainCAP-TACsUSP14RPN1BRD2BRD4HCT116 cellsRPN10RPN13HEK293T cellsBRD319S proteasome cap subunitsInhibitorinhibitorinhibit

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製品番号:
HY-181495
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