2. Apoptosis Immunology/Inflammation Epigenetics
  3. TNF Receptor Interleukin Related Epigenetic Reader Domain
  4. BRD4 Inhibitor-38

BRD4 Inhibitor-38 (Compound 25) is an orally active inhibitor of BRD4 with IC50 values of 3.64 μM and 0.12 μM against BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-38 also exhibits anti-inflammatory activity, with an IC50 value of 1.98 μM for inhibiting nitric oxide (NO) production.

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BRD4 Inhibitor-38 Chemical Structure

BRD4 Inhibitor-38 Chemical Structure

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BRD4 Inhibitor-38 Related Antibodies

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Description

BRD4 Inhibitor-38 (Compound 25) is an orally active inhibitor of BRD4 with IC50 values of 3.64 μM and 0.12 μM against BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-38 also exhibits anti-inflammatory activity, with an IC50 value of 1.98 μM for inhibiting nitric oxide (NO) production[1].

IC50 & Target[1]

BRD4 BD1

3.64 μM (IC50)

BRD4 BD2

0.12 μM (IC50)

In Vitro

BRD4 Inhibitor-38 (Compound 25) (2.5-20 μM; 2 h) exhibits anti-inflammatory activity in Raw 264.7 and THP-1 cells[1].

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

BRD4 Inhibitor-38 Related Antibodies

Real Time qPCR[1]

Cell Line: Raw 264.7, THP-1
Concentration: 2.5, 5, 10, 20 μM
Incubation Time: 2 h (stimulated with LPS (1 μg/mL) and LPS (100 ng/mL) + IFN-γ (20 ng/mL) for 6 h. note: Compound 25 were pre-treated for 2 h before stimulating with LPS for 6 h.)
Result: Inhibited the mRNA expression of LPS-induced IL-6 and TNF-α in a dependent manner.
In Vivo

BRD4 Inhibitor-38 (Compound 25) (25-100 mg/kg; p.o.; single dose) exhibits anti-inflammatory activity in a mouse model of acute inflammation induced by LPS (10mg/kg; Single dose) (HY-D1056)[1].

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

Animal Model: LPS-induced mouse model of acute inflammation[1].
Dosage: 25, 50, 100 mg/kg
Administration: Oral administration (p.o.)，single dose. After LPS treatment (10mg/kg; Single dose)
Result: Significantly inhibited the increase of inflammatory genes IL-6 and TNF-α at doses of 50 and 100 mg/kg.
Alleviated lung tissue edema, damage, and lung hemorrhage.
Mitigated kidney damage, significantly increased the proportion of normal renal tubules, improved the internal brush border structure, reduced renal interstitial inflammatory cell infiltration, and decreased the number of interstitial vacuoles at a dose of 100 mg/kg.
Molecular Weight

338.36

Formula

C19H18N2O4
SMILES

COC1=C2C(N=C(/C=C/C3=CC=C(OC)C=C3)NC2=O)=CC(OC)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BRD4 Inhibitor-38 Related Classifications

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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:

BRD4 Inhibitor-38TNF ReceptorInterleukin RelatedEpigenetic Reader DomainTumor Necrosis Factor ReceptorTNFRILRaw 264.7THP-1Anti-inflammatory activityInhibitorinhibitorinhibit

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