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GSK-114

Name: GSK-114
Brand: TargetMol
SKU: T22341
Price: 269 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.51%

货号 T22341Cas号 1301761-96-5

GSK 114 是口服有活性的、高选择性的TNNI3K 抑制剂 (IC50= 25 nM)。其中TNNI3K (又称 CARK) 是酪氨酸样激酶家族的成员，选择性在心脏组织中表达。它对 TNNI3K 的选择性是 B-Raf 激酶的 40 倍 (IC50= 1 µM)。

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GSK-114

一键复制产品信息

很棒

纯度: 99.51%

货号 T22341Cas号 1301761-96-5

规格	价格	库存
1 mg	¥ 269	现货
5 mg	¥ 629	现货
10 mg	¥ 987	现货
25 mg	¥ 1,980	现货
50 mg	¥ 3,290	现货
100 mg	¥ 4,730	现货
200 mg	¥ 6,590	现货
1 mL x 10 mM (in DMSO)	¥ 756	现货

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TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

实验操作小课堂

常见问题解答

选择批次:

纯度: 99.51%

颜色: 白色

性状: Solid

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资源下载:

COA LCMS HNMR 产品操作手册

产品介绍

GSK-114 AI Summary

GSK-114 is a potent inhibitor of human TNNI3K, with an IC50 value of 25.0 nM as determined by fluorescence polarization assay. It also exhibits inhibitory activity against B-Raf, with an IC50 of 1000.0 nM, showing a selectivity index of 40.0 for TNNI3K over B-Raf. The compound's inhibition of myc-TNNI3K has an IC50 of 100.0 nM. In rat studies, GSK-114 demonstrated an AUC/dose value of 0.18 hr.Kg/L when administered orally. The compound impacts cell viability differently across various cell types. In HEK293T cells, it generally promotes growth, with assay results ranging from 0.17 to 0.92. In U2OS cells, it also shows a positive effect on growth rates, albeit slightly lower, ranging from 0.39 to 0.84. In human fibroblast cells, the effects are mixed, with growth rates spanning from 0.29 to 0.69. Regarding thermal stability, GSK-114 shows diverse effects across different protein domains. Notable changes include: an increase of 0.23°C at domain M1-K294, a decrease of 0.02°C at domain M1-L298, an increase of 0.24°C at domain M1-S360, a significant increase of 3.42°C at domain S229-K512, and a decrease of 3.63°C at domain N44-E168. Overall, GSK-114 exhibits both stabilizing and destabilizing effects on protein thermal stability depending on the specific domain..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	GSK-114 is a selective inhibitor of TNNI3 interacting kinase (TNNI3K) with an IC50 of 25 nM, 40-fold significant bias for TNNI3K compared to B-Raf with an IC50 of 1000 nM, so GSK-114 has excellent Broad-spectrum kinase selectivity and sufficient oral exposure enable use in cellular and in vivo studies.
靶点活性	TNNI3K:25 nM

化学信息

分子量	417.48
分子式	C₁₉H₂₃N₅O₄S
CAS No.	1301761-96-5
Smiles	CNS(=O)(=O)c1ccc(N(C)C)c(Nc2ncnc3cc(OC)c(OC)cc23)c1
密度	no data available

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 5.5 mg/mL (13.17 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3953 mL	11.9766 mL	23.9532 mL	119.7662 mL
5 mM	0.4791 mL	2.3953 mL	4.7906 mL	23.9532 mL
10 mM	0.2395 mL	1.1977 mL	2.3953 mL	11.9766 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH₂O，那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 100 μL DMSO （母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。