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  3. L-Moses

L-Moses (Synonyms: L-45)

目录号: HY-101125 纯度: 99.97%
产品使用指南

L-Moses (L-45) 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 nM。

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L-Moses Chemical Structure

L-Moses Chemical Structure

CAS No. : 2079885-05-3

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

    L-Moses purchased from MCE. Usage Cited in: EMBO Rep. 2020 Mar 4;21(3):e48328.

    Inhibiting acetyltransferases CBP/P300 by TPOP146 (134 nM) or PCAF by L-45 (126 nM) for 24 h did not significantly decrease the K49-acetylated b-cat level in Tau-overexpressing N2a cells (n = 3 biological replicates each group)
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    L-Moses (L-45) is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM[1].

    IC50 & Target

    Brd

    126 nM (Kd)

    体外研究
    (In Vitro)

    L-Moses (L-45) disrupts PCAF-Brd histone H3.3 interaction in cells using a nanoBRET assay, and a co-crystal structure of L-Moses 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-Moses is also a potent ligand (isothermal titration calorimetry (ITC) KD 280 nM), is successfully obtained (PDB: 5TPX). L-Moses 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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    L-Moses (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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    360.46

    Formula

    C21H24N6

    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 33.33 mg/mL (92.47 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.7742 mL 13.8712 mL 27.7423 mL
    5 mM 0.5548 mL 2.7742 mL 5.5485 mL
    10 mM 0.2774 mL 1.3871 mL 2.7742 mL
    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    参考文献
    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    L-Moses
    目录号:
    HY-101125
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