L-45 dihydrochloride (L-Moses dihydrochloride)
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产品名称:
L-45 dihydrochloride (L-Moses dihydrochloride)
产品型号:
GOY-Y3517
产品展商:
谷研
产品文档:
无相关文档
发布时间:2023-05-08
简单介绍
L-45 dihydrochloride (L-Moses dihydrochloride)Soluble in DMSO
L-45 dihydrochloride (L-Moses dihydrochloride)
的详细介绍
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性能参数
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产品名称
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L-45 dihydrochloride (L-Moses dihydrochloride)
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规格
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5mg 10mg
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货号
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GOY-Y3517
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含量
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>98.00%
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CAS
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N/A
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别名
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N/A
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化学名
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N/A
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分子式
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C21H26Cl2N6
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分子量
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分子量 433.38
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溶解度
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Soluble in DMSO
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储存条件
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Store at -20°C
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General tips
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用途
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仅供科研
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价格
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电询
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详细内容
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L-45 dihydrochloride is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126±15 nM.
L-45 disrupts PCAF-Brd histone H3.3 interaction in cells using a nanoBRET assay, and a co-crystal structure of L-45 with the homologous Brd PfGCN5 from Plasmodium falciparum rationalizes the high selectivity for PCAF and GCN5 bromodomains. A structure using highly homologous (64 % identity) Brd from Plasmodium falciparum, PfGCN5, of which L-45 is also a potent ligand (isothermal titration calorimetry (ITC) KD 280 nM), is successfully obtained (PDB: 5TPX). L-45 binds in the acetylated lysines (KAc) -binding pocket of PfGCN (blue ribbon and sticks) and makes H-bonds (dotted lines) through the triazole to N1436 and the first of a network of four water molecules (red spheres)[1].
L-45 shows no observable cytotoxicity in peripheral blood mononuclear cells (PBMC), good cell-permeability, and metabolic stability in human and mouse liver microsomes, supporting its potential for in vivo use[1].
[1]. Moustakim M, et al. Discovery of a PCAF Bromodomain Chemical Probe. Angew Chem Int Ed Engl. 2017 Jan 16;56(3):827-831.
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