GSK-114 

GSK-114 is a highly selective, orally active TNNI3K inhibitor (IC₅₀= 25 nM). GSK-114 shows a 40-fold selectivity for TNNI3K over B-Raf kinase (IC₅₀= 1 µM). Cardiac troponin I-interacting kinase (TNNI3K or CARK) is a member of the tyrosine-like kinase family that is selectively expressed in heart tissue^[1].

At a concentration of 1 µM, GSK114 demonstrated an affinity for seven other kinases: ACK1, B-Raf, GAK, MEK5, PDGFRB, STK36, and ZAK^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GSK-114 affords the best balance of specificity and pharmacokinetics, demonstrating useful oral exposure (poDNAUC=0.18, C_max=130 ng/ml @ 2 mg/kg, t_1/2=3.6 hr, rat F_u=20.2%)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

417.48

C₁₉H₂₃N₅O₄S

1301761-96-5

Solid

Off-white to light yellow

O=S(NC)(C1=CC=C(N(C)C)C(NC2=C3C=C(OC)C(OC)=CC3=NC=N2)=C1)=O

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Lawhorn BG, et al. GSK114: A selective inhibitor for elucidating the biological role of TNNI3K. Bioorg Med Chem Lett. 2016;26(14):3355-3358.  [Content Brief]

  [2]. Asquith CRM, et al. New Insights into 4-Anilinoquinazolines as Inhibitors of Cardiac Troponin I-Interacting Kinase (TNNi3K). Molecules. 2020;25(7):1697. Published 2020 Apr 7.  [Content Brief]