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

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GSK-114 Property

storage temp.: Store at -20°C

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

DC Chemicals

Product number: 026104
Product name: GSK-114
Packaging: 001
Price: $650
Updated: 2021/12/16

DC Chemicals

Product number: 026104
Product name: GSK-114
Packaging: 002
Price: $1100
Updated: 2021/12/16

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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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GSK-114 Suppliers

China 15 United States 3 Global 18

ShangHai Biochempartner Co.,Ltd

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1301761-96-5, GSK-114Related Search:

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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

1301761-96-5