GSK-114
- Product Name
- GSK-114
- CAS No.
- 1301761-96-5
- Chemical Name
- GSK-114
- Synonyms
- GSK-114;GSK 114(freebase);3-((6,7-Dimethoxyquinazolin-4-yl)amino)-4-(dimethylamino)-N-methylbenzenesulfonamide;Benzenesulfonamide, 3-[(6,7-dimethoxy-4-quinazolinyl)amino]-4-(dimethylamino)-N-methyl-;Inhibitor,oral,selective,GSK 114,inhibit,heart tissue,cardiac diseases,GSK114,TNNI3K,GSK-114
- CBNumber
- CB63333736
- Molecular Formula
- C19H23N5O4S
- Formula Weight
- 417.48
- MOL File
- 1301761-96-5.mol
GSK-114 Property
- storage temp.
- Store at -20°C
- form
- Solid
- color
- Off-white to light yellow
N-Bromosuccinimide Price
- Product number
- 026104
- Product name
- GSK-114
- Packaging
- 001
- Price
- $650
- Updated
- 2021/12/16
- Product number
- 026104
- Product name
- GSK-114
- Packaging
- 002
- Price
- $1100
- Updated
- 2021/12/16
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.
GSK-114 Preparation Products And Raw materials
Raw materials
Preparation Products
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