Description
L-Moses (L-45) dihydrochloride is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM.
Product information
Molecular Weight: 433.38
Formula: C21H26Cl2N6
Chemical Name: (1S, 2S)-1-N, 1-N-dimethyl-2-N-(3-methyl-[1, 2, 4]triazolo[3, 4-a]phthalazin-6-yl)-1-phenylpropane-1, 2-diamine;dihydrochloride
Smiles: Cl.Cl.CN(C)[C@H]([C@H](C)NC1=NN2C(=NN=C2C)C2=CC=CC=C21)C1C=CC=CC=1
InChiKey: PCQCTBXCEBIRAC-YRRRDGBXSA-N
InChi: InChI=1S/C21H24N6.2ClH/c1-14(19(26(3)4)16-10-6-5-7-11-16)22-20-17-12-8-9-13-18(17)21-24-23-15(2)27(21)25-20;;/h5-14,19H,1-4H3,(H,22,25);2*1H/t14-,19+;;/m0../s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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 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-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 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).
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.
Products are for research use only. Not for human use.
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