1. Epigenetics
  2. Epigenetic Reader Domain
  3. L-45

L-45 (Synonyms: L-Moses)

製品番号: HY-101125
取扱説明書

L-45 is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126±15 nM.

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L-45 構造式

L-45 構造式

CAS 番号 : 2079885-05-3

容量 価格(税別) 在庫状況
5 mg USD 240 見積もりとリードタイムを求めるのご確認
10 mg USD 440 見積もりとリードタイムを求めるのご確認

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Other 在庫あり Forms of L-45:

Other Forms of L-45:

Top Publications Citing Use of Products

    L-45 purchased from MCE. Usage Cited in: EMBO Rep. 2020 Jan 13: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)
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    製品説明

    L-45 is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126±15 nM.

    IC50 & Target[1]

    Brd

    126 nM (Kd)

    体外実験

    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].

    体内実験

    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].

    分子量

    360.46

    分子式

    C₂₁H₂₄N₆

    CAS 番号

    2079885-05-3

    SMILES

    C[[email protected]@H]([[email protected]](C1=CC=CC=C1)N(C)C)NC(C2=C3C=CC=C2)=NN4C3=NN=C4C

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件

    Please store the product under the recommended conditions in the Certificate of Analysis.

    参考文献
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    Keywords:

    L-45L-MosesL45L 45Epigenetic Reader DomainInhibitorinhibitorinhibit

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    製品名:
    L-45
    製品番号:
    HY-101125
    数量:
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