JX 06 (Synonyms: NSC 402538) |
| カタログ番号GC50280 |
JX 06 は、PDK の強力な選択的共有結合阻害剤です。 JX 06 は、それぞれ 49 nM、101 nM、および 313 nM の IC50 で PDK1、PDK2、および PDK3 を阻害します。 JX 06 は、システイン残基に不可逆的に共有結合することにより、PDK1 活性を阻害します。 JX 06 は顕著な抗腫瘍活性を示します。
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Cas No.: 729-46-4
Sample solution is provided at 25 µL, 10mM.
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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
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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