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GSK-699 - CAS 2260944-68-9

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GSK-699 is a potent and cell-penetrating PCAF/GCN5 PROTAC.

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Molecular Formula

C45H51BrN8O7

Molecular Weight

895.86

GSK-699

- Specification
  - Related CAS
    
    2260944-69-0 ((3S,5S)-isomer)
    
    Purity
    
    ≥95%
    
    Solubility
    
    Soluble in DMSO
    
    Appearance
    
    Solid Powder
    
    Storage
    
    Store at 2-8°C for short term (days to weeks) or -20°C for long term (months to years)
    
    IUPAC Name
    
    4-[(3R,5R)-5-[(5-bromo-1-methyl-6-oxopyridazin-4-yl)amino]-1-methylpiperidin-3-yl]-N-[3-[4-[3-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxypropyl]-N-methylanilino]propyl]-N-methylbenzamide
    
    Synonyms
    
    GSK699; GSK 699; 4-((3R,5R)-5-((5-bromo-1-methyl-6-oxo-1,6-dihydropyridazin-4-yl)amino)-1-methylpiperidin-3-yl)-N-(3-((4-(3-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)propyl)phenyl)(methyl)amino)propyl)-N-methylbenzamide; Benzamide, 4-[(3R,5R)-5-[(5-bromo-1,6-dihydro-1-methyl-6-oxo-4-pyridazinyl)amino]-1-methyl-3-piperidinyl]-N-[3-[[4-[3-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]propyl]phenyl]methylamino]propyl]-N-methyl-; 4-[(3R,5R)-5-[(5-Bromo-1,6-dihydro-1-methyl-6-oxo-4-pyridazinyl)amino]-1-methyl-3-piperidinyl]-N-[3-[[4-[3-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]propyl]phenyl]methylamino]propyl]-N-methylbenzamide
- Properties
  - Density
    
    1.43±0.1 g/cm3
    
    InChI Key
    
    SARLMRHJAJBYBI-CIDUPMPKSA-N
    
    InChI
    
    InChI=1S/C45H51BrN8O7/c1-50-26-31(24-32(27-50)48-35-25-47-53(4)45(60)40(35)46)29-13-15-30(16-14-29)42(57)52(3)22-7-21-51(2)33-17-11-28(12-18-33)8-6-23-61-37-10-5-9-34-39(37)44(59)54(43(34)58)36-19-20-38(55)49-41(36)56/h5,9-18,25,31-32,36,48H,6-8,19-24,26-27H2,1-4H3,(H,49,55,56)/t31-,32+,36?/m0/s1
    
    Canonical SMILES
    
    CN1CC(CC(C1)NC2=C(C(=O)N(N=C2)C)Br)C3=CC=C(C=C3)C(=O)N(C)CCCN(C)C4=CC=C(C=C4)CCCOC5=CC=CC6=C5C(=O)N(C6=O)C7CCC(=O)NC7=O
- Reference Reading
  - 1. Modulating PCAF/GCN5 immune cell function through a PROTAC approach.
    
    Bassi, Z.I. ACS Chem. Biol. 13, 2862-2867 (2018).
    
    P300/CBP-associated factor (PCAF) and general control nonderepressible 5 (GCN5) are closely related epigenetic proteins, each containing an acetyltransferase domain and a bromodomain. Consistent with reported roles for these proteins in immune function, we find that PCAF-deficient macrophages exhibit a markedly reduced ability to produce cytokines upon stimulation with lipopolysaccharide (LPS). Investigating the potential to target this pathway pharmacologically, we show that chemical inhibition of the PCAF/GCN5 bromodomains is insufficient to recapitulate the diminished inflammatory response of PCAF-deficient immune cells. However, by generating the first PCAF/GCN5 proteolysis targeting chimera (PROTAC), we identify small molecules able to degrade PCAF/GCN5 and to potently modulate the expression of multiple inflammatory mediators in LPS-stimulated macrophages and dendritic cells. Our data illustrate the power of the PROTAC approach in the context of multidomain proteins, revealing a novel anti-inflammatory therapeutic opportunity for targeting PCAF/GCN5.

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