DW34
DW34 is an orally active pan-BRD4-D1 biased inhibitor with additional BRD4-D2 inhibitive activity. DW34 displays comparable inhibitive efficacy to I-BET151 (HY-13235) (EC50 = 0.16 μM) with low nanomolar EC50 values of 0.14 μM. DW34 significantly reduces liver inflammation induced by LPS (HY-D1056) and APAP (HY-66005) via reducing chemokine expression and cellular necrosis.
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- No. CAS: 2758171-54-7
- Fòrmula: C25H34N6O
- Peso molecular:434.58
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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BRD4-BD1 0.14 μM () |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MM1.S | EC50 |
<100 nM
Compound: 25;DW34
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Reduction in c-Myc expression in human MM1.S cells measured after 6 hrs by Western blot analysis
Reduction in c-Myc expression in human MM1.S cells measured after 6 hrs by Western blot analysis
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[PMID: 34236185] |
DW34 (Compound 3) (0.31-5 μM, 5 h) inhibits both CXCL1 and CCL2 expression induced by LPS (HY-D1056) (200 ng/mL, 4 h) in transformed sinusoidal endothelial cells (TSECs)[1].
DW34 (0.5-5 μM, 2 h) stabilizes BRD4 at comparable concentrations to I-BET151 (HY-13235) in HEK293T cells[1].
DW34 (0.1-200 μM, 4 h) shows good tolerance in transformed sinusoidal endothelial cells (TSECs)[1].
DW34 induces a toxicity profile with an EC50 of 90 nM in megakaryocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Transformed sinusoidal endothelial cells
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Concentration:0.31, 1.25 and 5 μM
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Incubation Time:1 h, following by 200 ng/mL LPS (HY-D1056) for 4 h
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Result:Decreased CXCL1 and CCL2 expression.
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Cell Line:HEK293T cells
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Concentration:0.5 and 5 μM
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Incubation Time:2 h
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Result:Stabilized BRD4 at comparable concentrations to I-BET151 (HY-13235 ) (EC50 = 0.16 μM).
| Species | Dose | Route | T1/2 | Cmax | AUC | CL/F |
|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 10.3 min | 0.43 μM | 0.64 μM·h | 28.2 L/h/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:N-acetyl-p-aminophenol (APAP) (HY-66005)-induced acute liver toxicity mice models (Wild-type C57BL/6J, male, 8-10 weeks)[1]
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Dosage:30 mg/kg
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Administration:Orally administration; 12 h after 1 h of 500 mg/kg APAP administration
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Result:Led to significant reduction of chemokine expression of CXCL1, CXCL2, and CCL2.
Reduced level of neutrophil marker Ly6G.
Reduced cellular necrosis (H&E staining).
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Animal Model:LPS (HY-D1056)-induced acute liver toxicity mice models (Wild-type C57BL/6J, male, 8-10 weeks)[1]
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Dosage:30 mg/kg
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Administration:Orally administration; 9 h (1 h before 8 h of 4 mg/kg LPS injection)
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Result:Induced a significant reduction in expression of the inflammatory chemokines CXCL1, CXCL2, and CCL2.
Reduced goblet cell.
Chemical Information
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No. CAS 2758171-54-7
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Peso molecular 434.58
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Fòrmula C25H34N6O
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SMILES
CC1=C(N(C2CCN(CC2)CCN(C)C)N=N1)C3=CC=CC(OC4=CC(C)=CC(C)=C4)=N3
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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)
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