JX 06 (Synonyms: NSC 402538) |
Catalog No.GC50280 |
JX 06 es un inhibidor potente, selectivo y covalente de PDK. JX 06 inhibe PDK1, PDK2 y PDK3 con IC50 de 49 nM, 101 nM y 313 nM, respectivamente. JX 06 inhibe la actividad de PDK1 a través de la unión covalente a un residuo de cisteína de manera irreversible. JX 06 muestra una actividad antitumoral significativa.
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Cas No.: 729-46-4
Sample solution is provided at 25 µL, 10mM.
Potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3 inhibitor (IC50 values are 49, 101 and 313 nM for PDK1, PDK2 and PDK3, respectively). Exhibits selectivity for PDK1/2/3 over PDK4 and a panel of 323 other kinases. Suppresses A549 lung cancer cell proliferation in vitro. Reduces tumor volume of A549 xenografts in mice.
Sun et al (2015) JX06 selectively inhibits pyruvate dehydrogenase kinase PDK1 by a covalent cysteine modification. Cancer Res. 75 4923 PMID:26483203
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