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L-45 dihydrochloride(L-Moses dihydrochloride)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
L-45 dihydrochloride(L-Moses dihydrochloride)图片
包装与价格：
包装价格(元)
5mg电议
10mg电议

产品介绍
L-45dihydrochloride是第一个有效的选择性p300/CBP相关因子(PCAF)溴结构域(Brd)抑制剂，Kd为126±15nM。
Canonical SMILESC[C@@H]([C@H](C1=CC=CC=C1)N(C)C)NC(C2=C3C=CC=C2)=NN4C3=NN=C4C.[H]Cl.[H]Cl
分子式C21H26Cl2N6
分子量433.38
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.