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  • DC Chemicals Limited
  • China
  • Product Name: GSK-114
  • Price: $650.0/100mg $1100.0/250mg $2000.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

1301761-96-5

1301761-96-5 structure
1301761-96-5 structure
  • Name: GSK-114
  • Chemical Name: GSK-114
  • CAS Number: 1301761-96-5
  • Molecular Formula:
  • Molecular Weight:
  • Catalog: Research Areas Cardiovascular Disease
  • Create Date: 2018-07-11 07:59:36
  • Modify Date: 2024-01-10 16:53:01
  • 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].

Name GSK-114
Description 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].
Related Catalog
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[2].
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%)[1].
References

[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.

[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.

No Any Chemical & Physical Properties