GSK-114
- Product NameGSK-114
- CAS1301761-96-5
- CBNumberCB63333736
- MFC19H23N5O4S
- MW417.48
- EINECS-0
- MDL NumberMFCD33029288
- MOL File1301761-96-5.mol
Chemical Properties
storage temp. | Store at -20°C |
GSK-114 Chemical Properties,Usage,Production
Biological Activity
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]. 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.Preparation Products And Raw materials
GSK-114 Suppliers
Global(19)Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
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+undefined-21-51877795 | ivan@atkchemical.com | China | 32686 | 60 | |
+1-781-999-5354 +1-00000000000 |
marketing@targetmol.com | United States | 19892 | 58 | |
86-571-88216897,88216896 13588875226 |
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+1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 | |
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021-58447131 13564518121 |
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021-51816796-820 13611835272 |
sales2@sunwaypharm.com | China | 44490 | 58 | |
18130062233 | 3362556465@qq.com | China | 8000 | 58 |
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