ZL0420

Names

[ Name ]:
ZL0420

[Synonym ]:
6-[(E)-(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-3,4-dihydro-2(1H)-quinolinone
2(1H)-Quinolinone, 6-[(E)-2-(2-amino-4-hydroxy-5-methylphenyl)diazenyl]-3,4-dihydro-

Biological Activity

[Description]:

ZL0420 is a potent, highly selective BRD4 inhibitor with IC50 of 27 and 32 nM for BRD4-BD1 and BRD4-BD2, respectively; displays selectivity over BRD2, BRD3, and BRDT (BRD2-BD1 and BRD2-BD2, IC50=803 and 1736 nM); disrupts the BRD4 complex with Pol II and histones, inhibits poly(I:C)-induced expression of innate immune genes IL6 and CIG5 in human small airway epithelial cells (hSAECs) (IC50=0.54 and 0.51 uM); blocks Poly(I:C)-induced inflammation and neutrophilia in vivo.

[References]

References 1. Tian B, et al. Cell Rep. 2018 Apr 24;23(4):1138-1151. 2. Liu Z, et al. Eur J Med Chem 2018 May 10;151:450-461. View Related Products by Target Bromodomain

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
645.9±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₆H₁₆N₄O₂

[ Molecular Weight ]:
296.324

[ Flash Point ]:
344.4±31.5 °C

[ Exact Mass ]:
296.127319

[ LogP ]:
2.19

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.704

[ Storage condition ]:
-20℃

Related Compounds

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