CRT0066101 is a potent and orally active PKD inhibitor with IC 50 values of 1 nM, 2.5 nM and 2 nM for PKD1 , PKD2 , and PKD3 , respectively. CRT0066101 is also a potent PIM2 inhibitor with an IC 50 of ~135.7 nM. CRT0066101 exhibits anti-inflammatory activity in mice LPS ( HY-D1056 )-induced lung injury models, and has anticancer effects.
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