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
- Molecular Weight:
- 417.48
- MDL Number:
- MFCD33029288
- MOL File:
- 1301761-96-5.mol
GSK-114 Chemical Properties,Uses,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
GSK-114 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | 2853530910@QQ.com | China | 8011 | 62 |
| Shanghai Chaolan Chemical Technology Center | QQ:65489617 15618227136 | info@SuperLan-chem.com | China | 9445 | 58 |
| DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9414 | 58 |
| ShangHai ChuanQian Chemcial Technique Centre | 15869524721 | 3525679403@qq.com | China | 3915 | 58 |
| Shanghai Sunway Pharmaceutical Technology Co.,Ltd. | 021-51816796-820 13611835272 | sales2@sunwaypharm.com | China | 44497 | 58 |
| Hefei Mokai Pharmaceutical Technology Co., Ltd | 18130062233 | 3362556465@qq.com | China | 8000 | 58 |