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| | GSK-114 Basic information |
| Product Name: | GSK-114 | | Synonyms: | GSK-114;Benzenesulfonamide, 3-[(6,7-dimethoxy-4-quinazolinyl)amino]-4-(dimethylamino)-N-methyl-;GSK 114(freebase);3-((6,7-Dimethoxyquinazolin-4-yl)amino)-4-(dimethylamino)-N-methylbenzenesulfonamide;Inhibitor,oral,selective,GSK 114,inhibit,heart tissue,cardiac diseases,GSK114,TNNI3K,GSK-114;GSK-114, 10 mM in DMSO | | CAS: | 1301761-96-5 | | MF: | C19H23N5O4S | | MW: | 417.48 | | EINECS: | | | Product Categories: | | | Mol File: | 1301761-96-5.mol |  |
| | GSK-114 Chemical Properties |
| storage temp. | Store at -20°C | | form | Solid | | color | Off-white to light yellow |
| | GSK-114 Usage And Synthesis |
| Uses | 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]. | | 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]. | | 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. |
| | GSK-114 Preparation Products And Raw materials |
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