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Biological Activity:
Chk1 inhibitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively. A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity.
References: online 1, 2, 3
JW Janetka et al, Inhibitors of Checkpoint Kinases: From discovery to the clinic. Curr. Opin. Drug Discov. & Devel. 2007, 10(4), 473-486.
S. Ashwell and S Zabludoff. DNA Damage Detection and Repair Pathways Recent Advances with Inhibitors of Checkpoint Kinases in Cancer Therapy. Clin. Cancer Res. 2008, 14(13), 4033-4037.
Chemical Name: (R)-2-Amino-2-cyclohexyl-N-[2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-5,6-dihydro-1H-[1,2]diazepino[4,5,6-cd]indol-8-yl]-acetamide dihydrochloride
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