ZL0420 |
Catalog No.GC19455 |
ZL0420은 BRD4 BD1에 대해 27nM, BRD4 BD2에 대해 32nM의 IC50 값을 갖는 강력하고 선택적 브로모도메인 함유 단백질 4(BRD4) 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2230496-80-5
Sample solution is provided at 25 µL, 10mM.
ZL0420 is a potent and selective BRD4 inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.
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].
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].
[1]. Liu Z, et al. Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. Eur J Med Chem. 2018 May 10;151:450-461.
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(Based on Reviews and 38 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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