GSK-114
- CAS No.
- 1301761-96-5
- Chemical Name:
- GSK-114
- Synonyms
- GSK-114;GSK 114(freebase);GSK-114, 10 mM in DMSO;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
- MSDS File:
- SDS
- TDS File:
- TDS
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H315-H319 |
| Precautionary statements | P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313 |
GSK-114 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0066770 | GSK-114 99.52% | 1301761-96-5 | 5mg | $103 | 2026-06-04 | Buy |
| ChemScene | CS-0066770 | GSK-114 99.52% | 1301761-96-5 | 10mg | $168 | 2026-06-04 | Buy |
| ChemScene | CS-0066770 | GSK-114 99.52% | 1301761-96-5 | 25mg | $341 | 2026-06-04 | Buy |
| ChemScene | CS-0066770 | GSK-114 99.52% | 1301761-96-5 | 50mg | $542 | 2026-06-04 | Buy |
| ChemScene | CS-0066770 | GSK-114 99.52% | 1301761-96-5 | 100mg | $867 | 2026-06-04 | Buy |
GSK-114 Chemical Properties, Uses, Production
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
Raw materials
Preparation Products
GSK-114 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 9920 | 65 |
| Shanghai Beckham Medical Technology Co., Ltd | 13816613772 | huahero21@sina.com | China | 2996 | 55 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9799 | 58 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 15026964105 | 2881489226@qq.com | China | 89667 | 60 |
| ShangHai Biochempartner Co.,Ltd | 177-54423994 17754423994 | 2853530910@QQ.com | China | 8000 | 62 |
| Shanghai Rechem science Co., Ltd. | 021-31433387 15618786686 | sales@rechemscience.com | China | 2970 | 58 |
| Shanghai Chaolan Chemical Technology Center | QQ：65489617 13301690235 | Sales@ATKchemical.com | China | 9699 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6288 | 58 |
| ShangHai ChuanQian Chemcial Technique Centre | 15869524721 | 3525679403@qq.com | China | 4565 | 58 |
