| MDL | - |
|---|---|
| Molecular Weight | 296.32 |
| Molecular Formula | C16H16N4O2 |
| SMILES | OC1=CC(N)=C(/N=N/C2=CC(CCC(N3)=O)=C3C=C2)C=C1C |
IC50: 27 nM (BRD4 BD1), 32 nM (BRD4 BD2) [1]
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.
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.
Solid
Room temperature in continental US; may vary elsewhere.
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
DMSO : 125 mg/mL ( 421.84 mM ; Need ultrasonic)
| 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 |
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