2. Epigenetics Apoptosis
  3. Epigenetic Reader Domain Necroptosis
  4. 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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DW34

DW34 構造式

CAS 番号 : 2758171-54-7

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DW34 関連抗体

Top Publications Citing Use of Products

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Brd BRPF1 BRPF2 BRPF3 BRD2 BRD3 BRD4 BRDT CECR2 BD1 BD2 BRD7 BRD9 BET BAZ

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製品説明

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[1].

IC50 & Target[1]

BRD4-BD1

0.14 μM ()

Cellular Effect
Cell Line Type Value Description References
MM1.S EC50
<100 nM
Compound: 25;DW34
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
[PMID: 34236185]
体外実験

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.

DW34 関連抗体

Real Time qPCR[1]

Cell Line: Transformed sinusoidal endothelial cells
Concentration: 0.31, 1.25 and 5 μM
Incubation Time: 1 h, following by 200 ng/mL LPS (HY-D1056) for 4 h
Result: Decreased CXCL1 and CCL2 expression.

Western Blot Analysis[1]

Cell Line: HEK293T cells
Concentration: 0.5 and 5 μM
Incubation Time: 2 h
Result: Stabilized BRD4 at comparable concentrations to I-BET151 (HY-13235 ) (EC50 = 0.16 μM).
Parmacokinetics
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
体内実験

DW34 (30 mg/kg, p.o., 9 or 12 h) significantly reduces liver inflammation induced by LPS (HY-D1056) and APAP (HY-66005) via reducing chemokine expression and cellular necrosis[1].

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

Animal Model: N-acetyl-p-aminophenol (APAP) (HY-66005)-induced acute liver toxicity mice models (Wild-type C57BL/6J, male, 8-10 weeks)[1]
Dosage: 30 mg/kg
Administration: Orally administration; 12 h after 1 h of 500 mg/kg APAP administration
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).
Animal Model: LPS (HY-D1056)-induced acute liver toxicity mice models (Wild-type C57BL/6J, male, 8-10 weeks)[1]
Dosage: 30 mg/kg
Administration: Orally administration; 9 h (1 h before 8 h of 4 mg/kg LPS injection)
Result: Induced a significant reduction in expression of the inflammatory chemokines CXCL1, CXCL2, and CCL2.
Reduced goblet cell.
分子量

434.58

分子式

C25H34N6O
CAS 番号
SMILES

CC1=C(N(C2CCN(CC2)CCN(C)C)N=N1)C3=CC=CC(OC4=CC(C)=CC(C)=C4)=N3
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
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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:

DW342758171-54-7DW 34DW-34Epigenetic Reader DomainNecroptosisBRD4 inhibitorLiver inflammationLPSAPAPHEK293T cellsTransformed sinusoidal endothelial cells (TSECs)Inhibitorinhibitorinhibit

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