GSK-114 is a potent and selective selective TNNI3K inhibitor (TNNI3 IC50 = 25nM; B-RafV600E IC50 = 1000 nM). GSK-114 displays significant bias (40-fold) for TNNI3K over B-Raf, exceptional broad spectrum kinase selectivity, and adequate oral exposure to enable its use in cellular and in vivo studies. Cardiac troponin I-interacting kinase (TNNI3K or CARK) is a member of the tyrosine-like kinase family that is selectively expressed in heart tissue. TNNI3K has been linked to the progression of dilated cardiomyopathy, cardiac hypertrophy, and ischemia/reperfusion injury using models that employ Tnni3k overexpressing or Tnni3k knockout animals.
MedKoo Cat#: 526660
Name: GSK-114
CAS#: 1301761-96-5 (free base)
Chemical Formula: C19H23N5O4S
Exact Mass: 417.1471
Molecular Weight: 417.48
Elemental Analysis: C, 54.66; H, 5.55; N, 16.78; O, 15.33; S, 7.68
The following data is based on the product molecular weight 417.48 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
