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DW34 is an orally bioactive pan-BRD4-D1-biased inhibitor that also exhibits BRD4-D2 activity. It demonstrates a low nanomolar inhibitory effect comparable to I-BET151 (EC50 value of 0.16 μM), with an EC50 value of 0.14 μM. DW34 significantly alleviates lipopolysaccharide (LPS)-induced liver inflammation and acetaminophen (APAP)-induced toxicity by reducing chemokine expression and cell necrosis.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | DW34 is an orally bioactive pan-BRD4-D1-biased inhibitor that also exhibits BRD4-D2 activity. It demonstrates a low nanomolar inhibitory effect comparable to I-BET151 (EC50 value of 0.16 μM), with an EC50 value of 0.14 μM. DW34 significantly alleviates lipopolysaccharide (LPS)-induced liver inflammation and acetaminophen (APAP)-induced toxicity by reducing chemokine expression and cell necrosis. |
| In vitro | DW34 (Compound 3) effectively inhibits the expression of CXCL1 and CCL2 in LPS-induced transformed sinusoidal endothelial cells (TSECs) at concentrations of 0.31-5 μM over 5 hours. At 0.5-5 μM over 2 hours, DW34 demonstrates a stabilization effect on BRD4 in HEK293T cells comparable to I-BET151. Furthermore, DW34 exhibits good tolerance in transformed sinusoidal endothelial cells (TSECs) at concentrations ranging from 0.1 to 200 μM over 4 hours. It also induces a toxic response in megakaryocytes with an EC50 value of 90 nM. |
| In vivo | When administered orally at 30 mg/kg for durations of 9 or 12 hours, DW34 effectively reduces LPS-induced liver inflammation and APAP-induced toxicity by decreasing chemokine expression and cellular necrosis. |
| Molecular Weight | 434.58 |
| Formula | C25H34N6O |
| Cas No. | 2758171-54-7 |
| Smiles | N1=NN(C(C=2N=C(OC=3C=C(C=C(C3)C)C)C=CC2)=C1C)C4CCN(CCN(C)C)CC4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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