GSK 329

Cat. No. 7637 提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent and selective TNNI3K inhibitor, orally bioavailable

化学名： N-[3,5-Dichloro-4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]-N'-[3-(trifluoromethyl)phenyl]urea

纯度： ≥98% (HPLC)

文献 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for GSK 329

GSK 329 is a potent and selective TNNI3K (cardiac troponin I-interacting kinase) inhibitor (IC₅₀ = 10 nM). It exhibits selectivity for TNNI3K over human VEGFR2 (40-fold), p38α (80-fold), B-Raf (>200-fold) and displays >100-fold selectivity over 80% of 185 kinases tested. In vivo, GSK 329 reduces infarct size, ROS levels, and p38 activation in a mouse model of ischemia/reperfusion cardiac injury. This compound is orally bioavailable.

技术数据 for GSK 329

分子量	472.25
公式	C₁₉H₁₄Cl₂F₃N₅O₂
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	1268490-12-5
PubChem ID	50997674
InChI Key	QOQADIYOLOHRAW-UHFFFAOYSA-N
Smiles	CNC1=CC(OC2=C(C=C(C=C2Cl)NC(NC3=CC(C(F)(F)F)=CC=C3)=O)Cl)=NC=N1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for GSK 329

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	47.23	100
	ethanol	9.45	20

制备储备液 for GSK 329

以下数据基于产品分子量 472.25。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	2.12 mL	10.59 mL	21.18 mL
5 mM	0.42 mL	2.12 mL	4.24 mL
10 mM	0.21 mL	1.06 mL	2.12 mL
50 mM	0.04 mL	0.21 mL	0.42 mL

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产品说明书 for GSK 329

分析证书/产品说明书

化学品安全技术说明书

参考文献 for GSK 329

参考文献是支持产品生物活性的出版物。

Patterson et al (2021) Identification of diarylurea inhibitors of the cardiac-specific kinase TNNI3K by designing selectivity against VEGFR2, p38a, and B-Raf. J.Med.Chem. 64 15651 PMID: 34699203

Vagnozzi et al (2013) Inhibition of the cardiomyocyte-specific kinase TNNI3K limits oxidative stress, injury, and adverse remodeling in the ischemic heart. Sci.Transl.Med. 5 207ra141 PMID: 24132636

If you know of a relevant reference for GSK 329, please let us know.

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关键词: GSK 329, GSK 329 supplier, GSK329, potent, selective, TNNI3K, inhibitors, inhibiTS, orally, bioavailable, kinases, MAPK, ischemia/reperfusion, cardiac, injury, in, vivo, Other, 7637, Tocris Bioscience

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该领域的文献

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。

MAPK Signaling Scientific Review

MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.