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ZL0454

Chemical Structure : ZL0454

CAS No.: 2229042-77-5

ZL0454 (ZL-0454;ZL 0454)

Catalog No.: PC-35097Not For Human Use, Lab Use Only.

ZL0454 is a potent, highly selective small-molecule BRD4 inhibitor with IC50 of 49 and 32 nM for BRD4-BD1 and BRD4-BD2, respectively.

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Biological Activity

ZL0454 is a potent, highly selective small-molecule BRD4 inhibitor with IC50 of 49 and 32 nM for BRD4-BD1 and BRD4-BD2, respectively.
ZL0454 displays selectivity over BRD2, BRD3, and BRDT( BRD2-BD1 and BRD2-BD2, IC50=772 and 1836 nM).
ZL0454 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=0.62 and 0.57 uM).
ZL0454 blocks Poly(I:C)-induced inflammation and neutrophilia in vivo.

Physicochemical Properties

M.Wt 374.459
Formula C18H22N4O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(E)-4-((2-amino-4-hydroxy-5-methylphenyl)diazenyl)-N-cyclopentylbenzenesulfonamide

References

1. Tian B, et al. Cell Rep. 2018 Apr 24;23(4):1138-1151.

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