GSK983

CAS No. 827591-02-6

GSK983( GSK-983 | GSK 983 )

Catalog No. M16075 CAS No. 827591-02-6

GSK983 (GSK-983) is a potent, cell penetrant PCAF/GCN5 PROTAC, induces concentration-dependent degradation of PCAF and GCN5 in THP1 cells with DC50 value of 1.5 nM and 3 nM, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GSK983
  • Note
    Research use only, not for human use.
  • Brief Description
    GSK983 (GSK-983) is a potent, cell penetrant PCAF/GCN5 PROTAC, induces concentration-dependent degradation of PCAF and GCN5 in THP1 cells with DC50 value of 1.5 nM and 3 nM, respectively.
  • Description
    GSK983 (GSK-983) is a potent, cell penetrant PCAF/GCN5 PROTAC, induces concentration-dependent degradation of PCAF and GCN5 in THP1 cells with DC50 value of 1.5 nM and 3 nM, respectively; also potently induces robust and concentration-dependent degradation of PCAF and GCN5 in both macrophages and monocyte-derived dendritic cells (DCs), potently modulate the expression of multiple inflammatory mediators in LPS-stimulated macrophages and dendritic cells.
  • In Vitro
    RT-PCR Cell Line:W12, HKC cells Concentration:10, 100 nM Incubation Time:24, 48 h Result:Induced the expression of interferon-stimulated genes in infected and immortalized cells, increased the gene expression of CSF2, IFIT1 (ISG56), IL6, ISG15, OAS1, OAS2, OASL and TNFSF10 (TRAIL).
  • In Vivo
    ——
  • Synonyms
    GSK-983 | GSK 983
  • Pathway
    PROTACs
  • Target
    PROTAC
  • Recptor
    PROTAC
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    827591-02-6
  • Formula Weight
    895.856
  • Molecular Formula
    C45H51BrN8O7
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : ≥ 10 mg/mL (30.69 mM)
  • SMILES
    O=C(N[C@H]1C(NC2=C3C=C(Cl)C=C2)=C3CCC1)C4=NC=CC=C4
  • Chemical Name
    4-(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

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Bassi ZI, et al. ACS Chem Biol. 2018 Oct 19;13(10):2862-2867.
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