ChemicalBook > CAS DataBase List > GSK-114

GSK-114

Product Name
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
Formula Weight
417.48
MOL File
1301761-96-5.mol
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GSK-114 Property

storage temp. 
Store at -20°C
form 
Solid
color 
Off-white to light yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

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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

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

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GSK-114 Suppliers

China 24 United States 3 Global 27
Shanghai Beckham Medical Technology Co., Ltd
Tel
13816613772
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QQ: 12922499
Email
huahero21@sina.com
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China
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2536
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Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
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China
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9803
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58
Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71615
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60
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
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Shanghai Rechem science Co., Ltd.
Tel
021-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
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China
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2962
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Shanghai Chaolan Chemical Technology Center
Tel
021-QQ：65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
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China
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9024
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TargetMol Chemicals Inc.
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+1-781-999-5354; +17819995354
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marketing@targetmol.com
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United States
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32469
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HANGZHOU CLAP TECHNOLOGY CO.,LTD
Tel
86-571-88216897,88216896 13588875226
Fax
86-571-88216895
Email
sales@hzclap.com
Country
CHINA
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6312
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ShangHai ChuanQian Chemcial Technique Centre
Tel
15869524721
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3525679403@qq.com
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China
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4998
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Shanghai Sunway Pharmaceutical Technology Co.,Ltd.
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021-51816796-820 13611835272
Fax
021-5161 3951
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sales2@sunwaypharm.com
Country
China
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44112
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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
  • GSK-114, 10 mM in DMSO
  • 1301761-96-5