1316059-00-3
Chemical Structure
GSK854
- CAS No.: 1316059-00-3
- Formula:C18H19ClN6O4S2
- Molecular Weight:482.96
IUPAC Name: 3-((6-((5-chloropyridin-2-yl)amino)pyrimidin-4-yl)amino)-4-(ethylsulfonyl)-N-methylbenzenesulfonamide
InChIKey: OEDGERSSZUMLBI-UHFFFAOYSA-N
SMILES: O=S(C1=CC=C(C(NC2=NC=NC(NC3=NC=C(C=C3)Cl)=C2)=C1)S(=O)(CC)=O)(NC)=O
Biological Activity: GSK854 is a TNNI3K inhibitor. GSK854 binds to the DFG-out conformation of the ATP-binding site and forms hydrogen bonds with the hinge and gatekeeper. GSK854 reduces mitochondrial superoxide production, ROS, and p38 MAPK activation, and protects mitochondrial membrane potential and cardiac function. GSK854 can be used in research on ischemia/reperfusion cardiac injury, heart failure, acute coronary syndrome, and ischemic heart disease[1][2][3][4][5][6].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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GSK854 | 98.40% | GSK854 is a TNNI3K inhibitor. GSK854 binds to the DFG-out conformation of the ATP-binding site and forms hydrogen bonds with the hinge and gatekeeper. GSK854 reduces mitochondrial superoxide production, ROS, and p38 MAPK activation, and protects mitochondrial membrane potential and cardiac function. GSK854 can be used in research on ischemia/reperfusion cardiac injury, heart failure, acute coronary syndrome, and ischemic heart disease. | ||||||||||||||||||||
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References
- [1]. Patterson JR, et al. Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity Against VEGFR2, p38α, and B-Raf. Journal of medicinal chemistry. 2021 Nov 11;64(21):15651-15670. [Content Brief]
- [2]. Philp J, et al. 4,6-Diaminopyrimidines as Highly Preferred Troponin I-Interacting Kinase (TNNI3K) Inhibitors. Journal of medicinal chemistry. 2018 Apr 12;61(7):3076-3088. [Content Brief]
- [3]. Bergmark BA, et al. Acute coronary syndromes. Lancet (London, England). 2022 Apr 02;399(10332):1347-1358.
- [4]. Chen K, et al. Design and synthesis of 4-azaindoles derivatives: targeting the cardiac troponin I-interacting kinase (TNNI3K). Bioorganic & medicinal chemistry. 2025 Dec 15;131:118395.
- [5]. Pang H, et al. Discovery of novel TNNI3K inhibitor suppresses pyroptosis and apoptosis in murine myocardial infarction injury. European journal of medicinal chemistry. 2020 Jul 01;197:112314.
- [6]. Yang M, et al. Validation of an HPLC-MS method for simultaneous determination of seven troponin activators in human urine and serum for doping control. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2026 Sep 01;1281:125147.
