JX06 is a potent, selective and covalent inhibitor of PDK . JX06 inhibits PDK1 , PDK2 and PDK3 with IC 50 s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity.
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