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ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with nanomolar binding affinities to the bromodomains (BDs) of BRD4, exhibiting IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $35 | In Stock | |
5 mg | $58 | In Stock | |
10 mg | $103 | In Stock | |
25 mg | $208 | In Stock | |
50 mg | $358 | In Stock | |
100 mg | $509 | In Stock | |
200 mg | $678 | In Stock | |
1 mL x 10 mM (in DMSO) | $64 | In Stock |
Description | ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with nanomolar binding affinities to the bromodomains (BDs) of BRD4, exhibiting IC50 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 demonstrates potent efficacy in reducing airway inflammation with low toxicity in a mouse model, almost completely blocking the significant accumulation of neutrophils around 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 | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 59 mg/mL (199.11 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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