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  3. BET-IN-13

BET-IN-13 is a potent BET inhibitor with an IC50 value of 1.6 nM. BET-IN-13 reduces LPS-induced TNF-α, IL-1β, IL-6, and NOS2 mRNA expression levels. BET-IN-13 shows anti-inflammatory activity. BET-IN-13 has the potential for the research of acute liver injury.

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BET-IN-13

BET-IN-13 Estructura química

No. CAS : 2506823-08-9

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Descripciòn

BET-IN-13 is a potent BET inhibitor with an IC50 value of 1.6 nM. BET-IN-13 reduces LPS-induced TNF-α, IL-1β, IL-6, and NOS2 mRNA expression levels. BET-IN-13 shows anti-inflammatory activity. BET-IN-13 has the potential for the research of acute liver injury[1].

IC50 & Target[1]

BRD4 BD1

57.4 nM (IC50)

BRD4 BD2

44.4 nM (IC50)

BRD2 BD1

79.3 nM (IC50)

BRD2 BD2

27.5 nM (IC50)

BRD3 BD1

45.6 nM (IC50)

BRD3 BD2

18.9 nM (IC50)

BRDT BD1

87.0 nM (IC50)

BRDT BD2

43.4 nM (IC50)

In Vitro

BET-IN-13 (compound 28) (1.1, 3.3, 10 µM, 2+6 h) reduces LPS (500 ng/ml) induced TNF-α, IL-1β, IL-6 and NOS2 mRNA expression levels in RAW264.7 cells[1].

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

RT-PCR[1]

Cell Line: RAW264.7 cells
Concentration: 1.1, 3.3, 10 µM
Incubation Time: Pre-treated for 2 h before stimulating with LPS for 6 h
Result: Significantly reduced LPS (500 ng/ml) induced TNF-α, IL-1β, IL-6 and NOS2 mRNA expression levels in a dose-dependent manner.
In Vivo

BET-IN-13 (3 mg/kg; i.v.; once) shows good pharmacokinetic (PK) properties with a T1/2 of 0.69 h, AUCINF-obs of 609 h*ng/mL and Vss of 1717 mL/kg in mouse[1].
BET-IN-13 (37.5, 75 mg/kg; i.p.; once) reduces the inflammation and hepatic damage without obvious toxicity in PS/D-GalN(d-gaiactosamine)-induced acute liver failure (ALF) mouse[1].

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

Animal Model: 20-22g, Female C57BL/6J mice (LPS/D-GalN(d-gaiactosamine)-induced acute liver failure (ALF))[1]
Dosage: 37.5, 75 mg/kg
Administration: I.p.; once
Result: Reduced inflammatory responses associated with LPS/GalN-induced acute liver failure with the survival rate increased significantly to 69.2% for37.5 mg/kg and to 84.6% for 75 mg/kg.
Peso molecular

497.56

Fòrmula

C28H23N3O4S

No. CAS
SMILES

CC1=C2C(NC=C3CN(C4=C(C(N32)=C1)C=C(C=C4)CS(C)(=O)=O)C(C5=CC=C6C=CC=CC6=C5)=O)=O

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

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Referencias
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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.

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Inquiry Information

Nombre del producto:
BET-IN-13
Cat. No.:
HY-152213
Cantidad:
MCE Japan Authorized Agent: