J594
J594 is a BRD4 molecular glue degrader targeting RNF126, with DC50 values of 0.077 μM (long-form BRD4 in HEK293T cells) and 0.26 μM (short-form BRD4 in HEK293T cells), respectively. J594 induces proteasome- and RNF126-dependent degradation of BRD4.
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- CAS No.: 3036531-21-9
- Formule: C34H32Cl2N6O4S
- Masse moléculaire:691.63
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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
Description
IC50 & Target
[1]|
BRD4 |
RNF126 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | DC50 |
0.077 μM
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Degradation of long BRD4 isoform in human HEK293T cells assessed by Western blotting after 16 h of treatment.
Degradation of long BRD4 isoform in human HEK293T cells assessed by Western blotting after 16 h of treatment.
|
41867716 |
| HEK-293T | DC50 |
0.26 μM
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Degradation of short BRD4 isoform in human HEK293T cells assessed by Western blotting after 16 h of treatment.
Degradation of short BRD4 isoform in human HEK293T cells assessed by Western blotting after 16 h of treatment.
|
41867716 |
In Vitro
J594 (0.0001-50 μM; 30 min) covalently binds to purified RNF126 protein in a dose-dependent manner, as demonstrated by competition assays with IA-rhodamine labeling[1].
J594 (0.01-10 μM; 16 h) potently and selectively degrades both long and short isoforms of BRD4 in a proteasome-dependent manner in HEK293T cells, with DC50 values of 0.077 μM and 0.26 μM, respectively[1].
J594 (0.1-1 μM; 10 h)-mediated BRD4 degradation depends on RNF126, as the degradation of both long and short BRD4 isoforms in HEK293T cells is significantly inhibited in RNF126-knockout cells compared with wild-type cells[1].
J594 (1 μM; 24 h) exhibits high target selectivity in MDA-MB-231 cells, where BRD4 is the major protein significantly downregulated[1].
J594 (0.1-10 μM; 24 h) exhibits only extremely low cytotoxicity in HEK293T, OVISE and MDA-MB-231 cells[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:0.01, 0.1, 0.5, 1, 2.5, 5, 10 μM
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Incubation Time:16 h
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Result:Induced dose-dependent degradation of both long and short BRD4 isoforms, with no appreciable loss of BRD2 or BRD3.
Achieved DC50 of 0.077 μM for long BRD4 and 0.26 μM for short BRD4.
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Cell Line:RNF126 wild-type and knockout HEK293T cells
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Concentration:0.1, 1 μM
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Incubation Time:10 h
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Result:Induced significant degradation of both long and short BRD4 isoforms in RNF126 wild-type HEK293T cells.
Showed significantly attenuated BRD4 degradation in RNF126 knockout HEK293T cells.
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Cell Line:HEK293T, OVISE ovarian cancer, and MDA-MB-231 breast cancer cells
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Concentration:0.1, 1, 10 μM
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Incubation Time:24 h
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Result:Showed minimal effects on cell viability across the tested concentration range in all three cell lines.
Chemical Information
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CAS No. 3036531-21-9
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Masse moléculaire 691.63
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Formule C34H32Cl2N6O4S
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SMILES
CC1=NN=C2N1C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N[C@H]2CC(N[C@H]5C[C@H](NC(/C=C/C(C6=C(Cl)C=C(OC)C=C6)=O)=O)C5)=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)
J594 Related Classifications
HY-187457 Related Classifications
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