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Home - Products - MAPK/ERK Signaling - MEK - GSK-114

GSK-114

CAS No. 1301761-96-5

GSK-114( GSK114 )

Catalog No. M11212 CAS No. 1301761-96-5

GSK-114 is a potent, selective TNNI3K inhibitor with IC50 of 25 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GSK-114
  • Note
    Research use only, not for human use.
  • Brief Description
    GSK-114 is a potent, selective TNNI3K inhibitor with IC50 of 25 nM.
  • Description
    GSK-114 is a potent, selective TNNI3K inhibitor with IC50 of 25 nM, dispalys 40-fold over B-Raf, exceptional broad spectrum kinase selectivity (IC50>1,000 nM, 99% of kinases, 291/294); has adequate oral exposure to enable its use in cellular and in vivo studies.
  • In Vitro
    At a concentration of 1 μM, GSK114 demonstrated an affinity for seven other kinases: ACK1, B-Raf, GAK, MEK5, PDGFRB, STK36, and ZAK.
  • In Vivo
    GSK-114 affords the best balance of specificity and pharmacokinetics, demonstrating useful oral exposure (poDNAUC=0.18, Cmax=130 ng/ml @ 2 mg/kg, t1/2=3.6 hr, rat Fu=20.2%).
  • Synonyms
    GSK114
  • Pathway
    MAPK/ERK Signaling
  • Target
    MEK
  • Recptor
    MEK
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1301761-96-5
  • Formula Weight
    417.484
  • Molecular Formula
    C19H23N5O4S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 5.95 mg/mL (14.25 mM)
  • SMILES
    O=S(C1=CC=C(N(C)C)C(NC2=C3C=C(OC)C(OC)=CC3=NC=N2)=C1)(NC)=O
  • Chemical Name
    3-((6,7-dimethoxyquinazolin-4-yl)amino)-4-(dimethylamino)-N-methylbenzenesulfonamide

Shipping & Storage Information

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

Reference

1. Lawhorn BG, et al. Bioorg Med Chem Lett. 2016 Jul 15;26(14):3355-8.
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