2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. SJH1-51B

SJH1-51B is a SKP1-recruiting BRD4 PROTAC degrader. SJH1-51B binds to SKP1 in the SKP1-FBXO7-CUL1-RBX1 complex, but shows no or weak binding to monomeric SKP1. SJH1-51B induces proteasome- and SKP1-dependent degradation of BRD4, and this degradation process relies on the neddylation modification of Cullin-RING E3 ligase. SJH1-51B induces proteasome-mediated degradation of the short isoform of BRD4 in non-cancer cells, while it induces proteasome-mediated degradation of both the long and short isoforms of BRD4 in breast cancer cells. SJH1-51B can be used for breast cancer research.
(Pink: BET ligand (HY-78695); Blue: SKP1 ligand (HY-175905); Black: linker).

For research use only. We do not sell to patients.

SJH1-51B

SJH1-51B Chemical Structure

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SJH1-51B Related Antibodies

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Description

SJH1-51B is a SKP1-recruiting BRD4 PROTAC degrader. SJH1-51B binds to SKP1 in the SKP1-FBXO7-CUL1-RBX1 complex, but shows no or weak binding to monomeric SKP1. SJH1-51B induces proteasome- and SKP1-dependent degradation of BRD4, and this degradation process relies on the neddylation modification of Cullin-RING E3 ligase. SJH1-51B induces proteasome-mediated degradation of the short isoform of BRD4 in non-cancer cells, while it induces proteasome-mediated degradation of both the long and short isoforms of BRD4 in breast cancer cells. SJH1-51B can be used for breast cancer research[1]. (Pink: BET ligand (HY-78695); Blue: SKP1 ligand (HY-175905); Black: linker).

IC50 & Target[1]

BRD4

 

SKP1​

 

In Vitro

SJH1-51B (0.1-10 μM; 24 h) dose-dependently degrades the short isoform of BRD4 in HEK293T cells, with the most robust degradation at 10 μM, but does not affect the long BRD4 isoform[1].
SJH1-51B (0.1-10 μM; 24 h) dose-dependently degrades both the long and short isoforms of BRD4 in MDA-MB-231 cells, with the most robust degradation at 10 μM[1].

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

SJH1-51B Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293T cells
Concentration: 0.1, 1, 5, 10 μM
Incubation Time: 24 h
Result: Reduced short BRD4 levels to ~95% of vehicle control at 0.1 μM.
Reduced short BRD4 levels to ~50% of vehicle control at 1 μM.
Reduced short BRD4 levels to ~60% of vehicle control at 5 μM.
Reduced short BRD4 levels to ~20% of vehicle control at 10 μM.
Did not degrade the long BRD4 isoform.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 breast cancer cells
Concentration: 0.1, 1, 5, 10 μM
Incubation Time: 24 h
Result: Reduced long BRD4 levels to ~80% and short BRD4 levels to ~85% of vehicle control at 0.1 μM.
Reduced long BRD4 levels to ~80% and short BRD4 levels to ~70% of vehicle control at 1 μM.
Reduced long BRD4 levels to ~50% and short BRD4 levels to ~60% of vehicle control at 5 μM.
Reduced long BRD4 levels to ~30% and short BRD4 levels to ~10% of vehicle control at 10 μM.
Molecular Weight

784.41

Formula

C42H50ClN7O4S
SMILES

O=C(NCCCCNC(C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1)=O)CCCOC5=CC=CC(CC6CCN(C(C=C)=O)CC6)=C5
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SJH1-51B Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SJH1-51BPROTACsEpigenetic Reader Domainbreast cancerBRD4MDA-MB-231 cellsproteasomeCullin-RING E3 ligasesSKP1-FBXO7-CUL1-RBX1 complexSKP1breast cancer cellsNEDDylationHEK293T cellsInhibitorinhibitorinhibit

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