A BRD4 inhibitor; inhibits BD1 and BD2 in BRD4 (IC50s = 27 and 32 nM

ZL0420 – 10 mg

Brand:
Cayman
CAS:
2229039-45-4
Storage:
-20
UN-No:
Non-Hazardous - /

ZL0420 is an inhibitor of bromodomain 1 (BD1) and BD2 in bromodomain-containing protein 4 (BRD4; IC50s = 27 and 32 nM, respectively).{52770} It is selective for BD1 and BD2 in BRD4 over BD1 in BRD2, BRD3, and BRDT (IC50s = 803, 2,275, and 3,183 nM, respectively) and BD2 (IC50s = 1,736, 2,193, and 2,781 nM, respectively), as well as the bromodomain in CBP (IC50 = >10,000 nM). ZL0420 inhibits the expression of interferon-stimulated gene 54 (ISG54), ISG56, IL-8, and growth-regulated protein β (Groβ) induced by the toll-like receptor 3 (TLR3) agonist poly(I:C) by approximately 95% in human small airway epithelial cells. It also inhibits neutrophil infiltration around small- and medium-sized airways and reduces cytokine expression in lung tissue in a poly(I:C)-induced mouse model of acute airway inflammation when administered at a dose of 10 mg/kg.  

 

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SKU: 30741 - 10 mg Category:

Description

A BRD4 inhibitor; inhibits BD1 and BD2 in BRD4 (IC50s = 27 and 32 nM, respectively); selective for BD1 and BD2 in BRD4 over BD1 in BRD2, BRD3, and BRDT (IC50s = 803, 2,275, and 3,183 nM, respectively) and BD2 (IC50s = 1,736, 2,193, and 2,781 nM, respectively), as well as the bromodomain in CBP (IC50 = >10,000 nM); inhibits neutrophil infiltration around small- and medium-sized airways and reduces cytokine expression in lung tissue in a poly(I:C)-induced mouse model of acute airway inflammation at 10 mg/kg

Formal name: 6-[2-(2-amino-4-hydroxy-5-methylphenyl)diazenyl]-3,4-dihydro-2(1H)-quinolinone

Synonyms: 

Molecular weight: 296.3

CAS: 2229039-45-4

Purity: ≥98%

Formulation: A crystalline solid

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