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GSK4027 - CAS 2079896-25-4

Inquiry

GSK4027 is a potent and selective inhibitor of p300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) bromodomain (Ki = 1.4 nM; IC50 = 60 nM in a chromatin engagement assay).

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Molecular Formula

C17H21BrN4O

Molecular Weight

377.3

GSK4027

- Specification
  - Purity
    
    ≥95%
    
    Appearance
    
    Crystalline Solid
    
    IUPAC Name
    
    4-bromo-2-methyl-5-[[(3R,5R)-1-methyl-5-phenylpiperidin-3-yl]amino]pyridazin-3-one
    
    Synonyms
    
    4-bromo-2-methyl-5-[[(3R,5R)-1-methyl-5-phenyl-3-piperidinyl]amino]-3(2H)-pyridazinone
- Properties
  - InChI Key
    
    VZAFGXCWAWRULT-UONOGXRCSA-N
    
    InChI
    
    InChI=1S/C17H21BrN4O/c1-21-10-13(12-6-4-3-5-7-12)8-14(11-21)20-15-9-19-22(2)17(23)16(15)18/h3-7,9,13-14,20H,8,10-11H2,1-2H3/t13-,14+/m0/s1
    
    Canonical SMILES
    
    CN1CC(CC(C1)NC2=C(C(=O)N(N=C2)C)Br)C3=CC=CC=C3
- Reference Reading
  - 1. Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe
    
    Jameed Hussain, Jessica F Renaux, Anne-Marie Michon, Thomas G Hayhow, Peter D Craggs, David F Tough, Philip G Humphreys, Laurie Gordon, Katherine L Jones, Matthew Lindon, Rab K Prinjha, Chun-Wa Chung, Colin J Suckling, Paola Grandi, Paul Bamborough J Med Chem . 2017 Jan 26;60(2):695-709. doi: 10.1021/acs.jmedchem.6b01566.
    
    p300/CREB binding protein associated factor (PCAF/KAT2B) and general control nonderepressible 5 (GCN5/KAT2A) are multidomain proteins that have been implicated in retroviral infection, inflammation pathways, and cancer development. However, outside of viral replication, little is known about the dependence of these effects on the C-terminal bromodomain. Herein, we report GSK4027 as a chemical probe for the PCAF/GCN5 bromodomain, together with GSK4028 as an enantiomeric negative control. The probe was optimized from a weakly potent, nonselective pyridazinone hit to deliver high potency for the PCAF/GCN5 bromodomain, high solubility, cellular target engagement, and ≥18000-fold selectivity over the BET family, together with ≥70-fold selectivity over the wider bromodomain families.
- Preparing Stock Solutions
  - ConcentrationVolumeMass 1 mg 5 mg 10 mg
    
    1 mM 2.6506 mL 13.2528 mL 26.5055 mL
    
    5 mM 0.5301 mL 2.6506 mL 5.3011 mL
    
    10 mM 0.2651 mL 1.3253 mL 2.6506 mL

ConcentrationVolumeMass	1 mg	5 mg	10 mg
1 mM	2.6506 mL	13.2528 mL	26.5055 mL
5 mM	0.5301 mL	2.6506 mL	5.3011 mL
10 mM	0.2651 mL	1.3253 mL	2.6506 mL

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