Powder: -20°C for 3 years | In solvent: -80°C for 1 year
L-45 is the first potent and cell-active bromodomain (Brd) inhibitor of p300/CBP-associated factor (PCAF) (Kd: 126±15 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 8-10 weeks | $ 882.00 | |
50 mg | 8-10 weeks | $ 1,170.00 | |
100 mg | 8-10 weeks | $ 1,770.00 |
Description | L-45 is the first potent and cell-active bromodomain (Brd) inhibitor of p300/CBP-associated factor (PCAF) (Kd: 126±15 nM). |
Targets&IC50 | BRD:126 nM (kd) |
In vitro | 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). 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 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 [1]. |
In vivo | In human and mouse liver microsomes, L-45 displays no observable cytotoxicity in peripheral blood mononuclear cells (PBMC), good cell-permeability, and metabolic stability. It also supports its potential for in vivo use[1]. |
Synonyms | L-45 |
Molecular Weight | 360.46 |
Formula | C21H24N6 |
CAS No. | 2079885-05-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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L-Moses 2079885-05-3 Others LMoses L 45 L-45 L45 L Moses inhibitor inhibit