2. Epigenetics
  3. Epigenetic Reader Domain
  4. ZL0420

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 210 In-stock
25 mg USD 420 In-stock
50 mg USD 720 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of ZL0420:

ZL0420 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

ZL0420 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

296.32

Formula

C16H16N4O2
CAS No.
Appearance

Solid

Color

Yellow to orange

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.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (421.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3747 mL 16.8736 mL 33.7473 mL 84.3682 mL
5 mM 0.6749 mL 3.3747 mL 6.7495 mL 16.8736 mL
10 mM 0.3375 mL 1.6874 mL 3.3747 mL 8.4368 mL
15 mM 0.2250 mL 1.1249 mL 2.2498 mL 5.6245 mL
20 mM 0.1687 mL 0.8437 mL 1.6874 mL 4.2184 mL
25 mM 0.1350 mL 0.6749 mL 1.3499 mL 3.3747 mL
30 mM 0.1125 mL 0.5625 mL 1.1249 mL 2.8123 mL
40 mM 0.0844 mL 0.4218 mL 0.8437 mL 2.1092 mL
50 mM 0.0675 mL 0.3375 mL 0.6749 mL 1.6874 mL
60 mM 0.0562 mL 0.2812 mL 0.5625 mL 1.4061 mL
80 mM 0.0422 mL 0.2109 mL 0.4218 mL 1.0546 mL
100 mM 0.0337 mL 0.1687 mL 0.3375 mL 0.8437 mL
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ZL0420 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZL04202230496-80-5ZL 0420ZL-0420Epigenetic Reader DomainInhibitorinhibitorinhibit

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