GSK-114 是一种高选择性的，具有口服活性的 TNNI3K 抑制剂 (IC50= 25 nM)。GSK-114 对 TNNI3K 的选择性是 B-Raf 激酶的 40 倍 (IC50= 1 µM)。TNNI3K (又称 CARK) 是酪氨酸样激酶家族的成员，在心脏组织中选择性表达。
货号:ajcx36614
CAS:1301761-96-5
分子式:C19H23N5O4S
分子量：417.48
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

[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.