SJ46420
SJ46420 is a BRD3 PROTAC degrader with a DC50 of 224 nM in U2OS cells. SJ46420 selectively mediates BRD3 degradation, exerts only partial effects on BRD2 and BRD4, and its activity is dependent on KLHDC2. SJ46420 is a prodrug variant of SJ46421 (HY-168634). SJ46420 can be used in the research of prostate cancer.
(Pink: BRD3 ligand (HY-13030); Blue: KLHDC2 ligand (HY-159973); Black: linker (HY-20797)).
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- Formule: C43H43ClN8O5S2
- Masse moléculaire:851.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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VHL |
BRD3 |
SJ46420 (0.001-10 μM; 24 h) potently and selectively degrades BRD3 in a KLHDC2-dependent manner across multiple cell lines, with the highest potency (DC50 = 224 nM) observed in KLHDC2-overexpressing U2OS knockout/rescue cells, and ~2.5- to 44-fold selectivity for BRD3 over BRD2 and BRD4 in different cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:wild-type U2OS cells, KLHDC2 knockout U2OS cells, KLHDC2 knockout/rescue U2OS cells, PC3 cells, 22Rv1 cells
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Concentration:5 μM (wild-type and KLHDC2 knockout U2OS cells); 1 μM (KLHDC2 knockout/rescue U2OS cells); 0.001-10 μM (dose-response assays in KLHDC2 knockout/rescue U2OS, PC3, and 22Rv1 cells); 1 μM (co-treatment with MLN4924)
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Incubation Time:24 h
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Result:Efficiently and selectively degraded BRD3, with only partial reductions in BRD2 and BRD4 levels in wild-type U2OS cells.
Showed no degradation of BRD proteins in KLHDC2 knockout U2OS cells.
Induced the most substantial downregulation of BRD3, with lesser reductions in BRD4 and BRD2 in KLHDC2 knockout/rescue U2OS cells.
Yielded a DC50 of 224 nM and Dmax of 99.9% for BRD3, a DC50 of 616 nM and Dmax of 99.3% for BRD2, and a DC50 of 548 nM and Dmax of 99.4% for BRD4 in KLHDC2 knockout/rescue U2OS cells.
Had a DC50 of 487 nM and Dmax of 99.9% for BRD3, with a DC50 >30,000 nM and Dmax of 19.5% for BRD2, and a DC50 of 13,729 nM and Dmax of 59.5% for BRD4 in PC3 cells.
Had a DC50 of 458 nM and Dmax of 93.7% for BRD3, with a DC50 >100,000 nM and Dmax of 0.0% for BRD2, and a DC50 of 20,071 nM and Dmax of 30.0% for BRD4 in 22Rv1 cells.
Stabilized BRD3 when co-treated with MLN4924, confirming CRL-dependence of the degradation.
Chemical Information
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Masse moléculaire 851.44
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Formule C43H43ClN8O5S2
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SMILES
O=C(OC)CNC(CC1=CSC(C2=CC=C3C=CC=C(OCCN4CCN(C(C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5)=O)CC4)C3=C2)=N1)=O
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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)
SJ46420 Related Classifications
HY-168635 Related Classifications
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