GSK 329

Pricing Availability   Qty
Description: Potent and selective TNNI3K inhibitor, orally bioavailable
Chemical Name: N-[3,5-Dichloro-4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]-N'-[3-(trifluoromethyl)phenyl]urea
Purity: ≥98% (HPLC)
Literature (1)

Biological Activity 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.

Technical Data for GSK 329

M. Wt 472.25
Formula C19H14Cl2F3N5O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1268490-12-5
PubChem ID 50997674
Smiles CNC1=CC(OC2=C(C=C(C=C2Cl)NC(NC3=CC(C(F)(F)F)=CC=C3)=O)Cl)=NC=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

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

Solubility Data for GSK 329

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 47.23 100
ethanol 9.45 20

Preparing Stock Solutions for GSK 329

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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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References for GSK 329

References are publications that support the biological activity of the product.

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

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Keywords: 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

Citations for GSK 329

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Literature in this Area

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MAPK Signaling Scientific Review

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.