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

L-45 dihydrochloride (Synonyms: L-Moses dihydrochloride)

Cat. No.: HY-101125A Purity: 99.38%
Handling Instructions

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.

For research use only. We do not sell to patients.

L-45 dihydrochloride Chemical Structure

L-45 dihydrochloride Chemical Structure

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5 mg USD 240 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of L-45 dihydrochloride:

Top Publications Citing Use of Products

Publications Citing Use of MCE L-45 dihydrochloride

    L-45 dihydrochloride 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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    Description

    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.

    IC50 & Target[1]

    Brd

    126 nM (Kd)

    In Vitro

    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].

    In Vivo

    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].

    Molecular Weight

    433.38

    Formula

    C₂₁H₂₆Cl₂N₆

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    References
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    Keywords:

    L-45L-MosesL45L 45Epigenetic Reader DomainInhibitorinhibitorinhibit

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    Product name:
    L-45 dihydrochloride
    Cat. No.:
    HY-101125A
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