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F1324 Sale

目录号 : GC36022

F1324 是一种有效、高亲和力的 BCL6 多肽抑制剂,IC50 值为 1 nM。

F1324 Chemical Structure

Cas No.:2607975-44-8

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Sample solution is provided at 25 µL, 10mM.

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产品描述

F1324 is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6) with an IC50 of 1 nM[1]. IC50: 1 nM (BCL6)[1]

[1]. Sakamoto K, et al. Discovery of high-affinity BCL6-binding peptide and its structure-activity relationship. Biochem Biophys Res Commun. 2017 Jan 8;482(2):310-316.

Chemical Properties

Cas No. 2607975-44-8 SDF
分子式 分子量
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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Research Update

Discovery of high-affinity BCL6-binding peptide and its structure-activity relationship

Biochem Biophys Res Commun 2017 Jan 8;482(2):310-316.PMID:27856253DOI:10.1016/j.bbrc.2016.11.060.

B cell lymphoma 6 (BCL6) is a transcriptional repressor that interacts with its corepressors BcoR and SMRT. Since this protein-protein interaction (PPI) induces activation and differentiation of B lymphocytes, BCL6 has been an attractive drug target for potential autoimmune disease treatments. Here we report a novel BCL6 inhibitory peptide, F1324 (Ac-LWYTDIRMSWRVP-OH), which we discovered using phage display technology; we also discuss this peptide's structure-activity relationship (SAR). For BCL6(5-129) binding, KD and IC50 values of F1324 were 0.57 nM and 1 nM according to the results of an SPR analysis and cell-free ELISA assay, respectively. In contrast, BcoR(Arg498-514Pro) and SMRT(Leu1422-Arg1438) exhibited relatively weak micromole-order binding to BCL6. Furthermore, Fusion protein AcGFP-F1324 transiently expressed in HEK293T cells inhibited intracellular PPI in cell-based M2H assay. By examination of the truncation and fragmentation of F1324, the C-terminal sequence WRVP, which is similar to the BcoR(509-512) sequence WVVP, was identified as being critical for BCL6 binding. In addition, subsequent single-crystal X-ray diffraction analysis of F1324/BCL6(5-129) complex revealed that the high affinity of F1324 was caused by effective interaction of its side chains while its main chain structure was similar to that of BcoR(Arg498-514Pro). To our knowledge, F1324 is the strongest BCL6-binding peptide yet reported.