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ZL0420 

Cat. No.: HY-112149 Purity: >98.0%
Handling Instructions

ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.

For research use only. We do not sell to patients.

ZL0420 Chemical Structure

ZL0420 Chemical Structure

CAS No. : 2230496-80-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 210 In-stock
Estimated Time of Arrival: December 31
25 mg USD 420 In-stock
Estimated Time of Arrival: December 31
50 mg USD 720 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Technical Information

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  • References

Description

ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.

IC50 & Target

IC50: 27 nM (BRD4 BD1), 32 nM (BRD4 BD2)[1]

In Vitro

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].

In Vivo

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].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (421.84 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3747 mL 16.8736 mL 33.7473 mL
5 mM 0.6749 mL 3.3747 mL 6.7495 mL
10 mM 0.3375 mL 1.6874 mL 3.3747 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.02 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.02 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

hSAECs are first pretreated with a series final concentrations of BRD4 inhibitors from 0.01 nM to 100 µM for 24 hours and are then added poly(I:C) at 10 µg/mL for another 4 hours prior to harvesting the cells. The harvested cells are first ished with PBS twice and then the total RNA is extracted using acid guanidinium phenol extraction. The total RNA is further reverse-transcribed for gene expression analysis by Q-RT-PCR[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]

C57BL/6 mice are pre-treated in the absence or presence of the ZL0420 [10 mg/kg body weight, via the intraperitoneal route] one day prior to poly(I:C) stimulation. The next day, animals are given another dose of ZL0420 immediately followed by intranasal (i.n.) administration of phosphate-buffered saline (PBS, 50 µL) or poly(I:C) (300 µg dissolved in 50 µL PBS). One day later, the mice are euthanized. The bronchoalveolar lavage fluid (BALF) and lung tissues of treated mice are collected for further analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

296.32

Formula

C₁₆H₁₆N₄O₂

CAS No.

2230496-80-5

SMILES

OC1=CC(N)=C(/N=N/C2=CC(CCC(N3)=O)=C3C=C2)C=C1C

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
ZL0420
Cat. No.:
HY-112149
Quantity:

ZL0420

Cat. No.: HY-112149