A TNNI3K inhibitor and sorafenib derivative
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GSK329

Item No. 40666

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3,5-dichloro-4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]-N′-[3-(trifluoromethyl)phenyl]-urea
CAS Number
1268490-12-5
Molecular Formula
C19H14Cl2F3N5O2
Formula Weight
472.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mLEthanol: Slightly soluble: 0.1-1 mg/mL
SMILES
O=C(NC1=CC(Cl)=C(C(Cl)=C1)OC2=NC=NC(NC)=C2)NC3=CC=CC(C(F)(F)F)=C3
InChi Code
InChI=1S/C19H14Cl2F3N5O2/c1-25-15-8-16(27-9-26-15)31-17-13(20)6-12(7-14(17)21)29-18(30)28-11-4-2-3-10(5-11)19(22,23)24/h2-9H,1H3,(H,25,26,27)(H2,28,29,30)
InChi Key
QOQADIYOLOHRAW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

    $372

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    Product Description

    GSK329 is an inhibitor of cardiac troponin I-interacting kinase (TNNI3K; IC50 = 10 nM) and a derivative of the multi-kinase inhibitor sorafenib (Item Nos. 10009644 | 35612).1 It is selective for TNNI3K over VEGFR2, p38α, and B-RAF (IC50s = 400, 800, and >2,000 nM, respectively). In vivo, GSK329 (2.75 mg/kg) reduces superoxide levels in isolated left ventricular tissues and infarct size in a mouse model of myocardial ischemia-reperfusion injury induced by left anterior descending (LAD) coronary artery occlusion.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Patterson, J.R., Graves, A.P., Stoy, P., et al. Identification of diarylurea inhibitors of the cardiac-specific kinase TNNI3K by designing selectivity against VEGFR2, p38α, and B-Raf. J. Med. Chem. 64(21), 15651-15670 (2021).

    2. Vagnozzi, R.J., Gatto, G.J., Jr., Kallander, L.S., et al. Inhibition of the cardiomyocyte-specific kinase TNNI3K limits oxidative stress, injury, and adverse remodeling in the ischemic heart. Sci. Transl. Med. 5(207), 207ra141 (2013).