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  3. L-45

L-45 (Synonyms: L-Moses)

Cat. No.: HY-101125
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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.

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

L-45 Chemical Structure

L-45 Chemical Structure

CAS No. : 2079885-05-3

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Description

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)

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].

Storage

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

References
Molecular Weight

360.46

Formula

C₂₁H₂₄N₆

CAS No.

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

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Room temperature in continental US; may vary elsewhere

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Cat. No.: HY-101125