RGNCY-0079 (Compound 43 TAO kinase inhibitor)

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Compound 43 selectively inhibit TAOK (Thousand -and -one amino acid kinases) 1 and 2 activity with IC50 of 11-15 nmole/L and is ATP competitive.  TAOK inhibition in centrosome-amplified SKBR3 or BT549 breast cancer cell models increases the mitotic population, the percentage of mitotic cells displaying amplified centrosomes and multipolar spindles, as well as inducing cell death and inhibiting cell growth. However, in non-tumorigenic and dividing bipolar MCF-10A breast cells can complete mitosis and proliferate in the presence of compound 43 as they are less dependent on TAOK activity.  Compound 43 is shown by live cell imaging to prolong the duration of mitosis in SKBR3 cells and reduce the percentage of cells exiting mitosis,whereas MCF-10A cells continue to divide and proliferate.  Compound 43 enhances centrosome declustering and mitotic disaster in cancer cells and may offer a new therapeutic option for breast cancer treatment where supernumerary centrosomes occur.

Systematic Name: N-(2-oxo-2-((1,2,3,4-tetrahydronaphthalen-1-yl)amino)ethyl)-[1,1'-biphenyl]-4-carboxamide

Formula: C25H24N2O2
Mol Wt:  384.48

PMID: 28830982

Reference:  Koo C-Y et al.  Targeting TAO Kinases Using a New Inhibitor Compound Delays Mitosis and Induces Mitotic Cell Death in Centrosome Amplified Breast Cancer Cells.  Mol Cancer Ther; 16(11) November 2017:2410-2421.

Tags: Small molecules, Cancer, breast cancer, Breast, RGNCY-0079, TAOK, mitosis, SKBR3, MCF-10A, compound 43