ZL0420 |
Catalog No.GC19455 |
ZL0420 est un inhibiteur puissant et sélectif de la protéine 4 contenant du bromodomaine (BRD4) avec des valeurs IC50 de 27 nM contre BRD4 BD1 et de 32 nM contre BRD4 BD2.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2230496-80-5
Sample solution is provided at 25 µL, 10mM.
ZL0420 is a potent and selective BRD4 inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.
ZL0420 is well docked into the acetyl-lysine (KAc) binding pocket of BRD4, forming key interactions including the critical hydrogen bonds with Asn140 directly and Tyr97 indirectly via a H2O molecule. ZL0420 exhibits submicromolar potency of inhibiting the TLR3-dependent innate immune gene program, including ISG54, ISG56, IL-8, and Groβ genes in cultured human small airway epithelial cells (hSAECs) with IC50s of 0.49-0.86 µM[1].
ZL0420 demonstrates potent efficacy reducing airway inflammation in a mouse model with low toxicity. ZL0420 displays high efficacy and almost completely blocks the profound accumulation of neutrophils around the small and medium sized airways induced by poly(I:C) administration[1].
[1]. Liu Z, et al. Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. Eur J Med Chem. 2018 May 10;151:450-461.
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(Based on Reviews and 38 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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