[CAS NO. 2230496-80-5]  ZL0420

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PRODUCTS SPECIFICATIONS [2230496-80-5]

Distributor
Catalog
AS945499
Brand
Arctom Scientific
CAS
2230496-80-5

DESCRIPTION [2230496-80-5]

Overview

MDL-
Molecular Weight296.32
Molecular FormulaC16H16N4O2
SMILESOC1=CC(N)=C(/N=N/C2=CC(CCC(N3)=O)=C3C=C2)C=C1C

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

Summary

ZL0420 is a potent and selective bromodomain-containing protein 4 ( BRD4 ) inhibitor with IC 50 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 H 2 O 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 IC 50 s of 0.49-0.86 µM [1] .

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


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] .

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


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


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 >> 40% PEG300 >> 5% Tween-80 >> 45% saline

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

  • 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

* All of the co-solvents are available by MCE.