>>Signaling Pathways>> Chromatin/Epigenetics>> Epigenetic Reader Domain>>ZL0420

ZL0420

Catalog No.GC19455

ZL0420은 BRD4 BD1에 대해 27nM, BRD4 BD2에 대해 32nM의 IC50 값을 갖는 강력하고 선택적 브로모도메인 함유 단백질 4(BRD4) 억제제입니다.

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ZL0420 Chemical Structure

Cas No.: 2230496-80-5

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$123.00
재고 있음
5mg
US$80.00
재고 있음
10mg
US$176.00
재고 있음
25mg
US$352.00
재고 있음
50mg
US$640.00
재고 있음

Tel:(909) 407-4943 Email: sales@glpbio.com

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Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

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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Average Rating: 5 ★★★★★ (Based on Reviews and 38 reference(s) in Google Scholar.)

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