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ZL0420

Catalog No. T6828   CAS 2229039-45-4

ZL0420 is a potent and selective bromodomain-containing protein 4 ( BRD4 ) inhibitor with nanomolar binding affinities to bromodomains (BDs) of BRD4. ZL0420 has IC 50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.

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ZL0420 Chemical Structure
ZL0420, CAS 2229039-45-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
5 mg In stock $ 97.00
10 mg In stock $ 172.00
25 mg In stock $ 347.00
50 mg In stock $ 597.00
100 mg In stock $ 849.00
200 mg In stock $ 1,130.00
1 mL * 10 mM (in DMSO) In stock $ 107.00
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Purity: 97.77%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description ZL0420 is a potent and selective bromodomain-containing protein 4 ( BRD4 ) inhibitor with nanomolar binding affinities to bromodomains (BDs) of BRD4. ZL0420 has IC 50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.
In vitro ZL0420 effectively binds to the acetyl-lysine (KAc) binding pocket of BRD4, establishing essential interactions, notably critical hydrogen bonds directly with Asn140 and indirectly with Tyr97 through a water molecule. It demonstrates submicromolar efficacy in suppressing the TLR3-dependent innate immune gene program, including ISG54, ISG56, IL-8, and Groβ genes in cultured human small airway epithelial cells (hSAECs), with IC50 values ranging from 0.49 to 0.86 μM [1].
In vivo ZL0420 displays potent efficacy reducing airway inflammation in a mouse model with low toxicity. ZL0420 displays highly potent and almost completely blocks the profound accumulation of neutrophils around the small and medium sized airways induced by poly(I:C) administration [1].
Molecular Weight 296.32
Formula C16H16N4O2
CAS No. 2229039-45-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 59 mg/mL (199.11 mM)

TargetMolReferences and Literature

1. Tian B, Liu Z, Litvinov J,et al.Efficacy of Novel Highly Specific Bromodomain-Containing Protein 4 Inhibitors in Innate Inflammation-Driven Airway Remodeling[J].Am J Respir Cell Mol Biol. 2019 Jan;60(1):68-83.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Kinase Inhibitor Library Epigenetics Compound Library Histone Modification Compound Library Anti-Aging Compound Library PPI Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Immunology/Inflammation Compound Library

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AU-15330 Physachenolide C MI-3 BI 2536 GNE-064 MZ 1 ZEN-3694 CPI-203

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Keywords

ZL0420 2229039-45-4 Chromatin/Epigenetic Epigenetic Reader Domain ZL 0420 inhibit (E/Z)-ZL0420 BRD4 airway inflammation immune response genes ZL-0420 BET bromodomains Inhibitor inhibitor

 

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