[CAS NO. 2079885-05-3] L-Moses
PRODUCTS SPECIFICATIONS [2079885-05-3]
DESCRIPTION [2079885-05-3]
Overview
| MDL | MFCD31563590 |
|---|---|
| Molecular Weight | 360.46 |
| Molecular Formula | C21H24N6 |
| SMILES | C[C@@H]([C@H](C1=CC=CC=C1)N(C)C)NC(C2=C3C=CC=C2)=NN4C3=NN=C4C |
1 Publications Citing Use of MCE
Summary
IC50 & Target
|
Brd 126 nM (Kd) |
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 Pf GCN5 from Plasmodium falciparum rationalizes the high selectivity for PCAF and GCN5 bromodomains. A structure using highly homologous (64 % identity) Brd from Plasmodium falciparum , Pf GCN5, 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 Pf GCN (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.
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.
Appearance
Solid
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 |
Solvent & Solubility
DMSO : 33.33 mg/mL ( 92.47 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
