RGNCY-0073 (PI-273 PI4KIIα inhibitor)

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PI-273 is the first small molecule inhibitor of PI4KIIα.  PI-273 inhibits PI4KIIα kinase activity (IC50 = 0.47 µM) and suppresses MCF-7 and T-47D cell proliferation.  Surface plasmon resonance and thermal shift assays indicate that PI-273 interacts directly with PI4KIIα.  Kinetic analysis demonstrated that PI-273 is a reversible competitive inhibitor with respect to the substrate PI which contrasts with most other PI kinase inhibitors that bind the ATP binding site.  PI-273 reduces PI4P content, cell viability and AKT signalling in wild type MCF-7 cells but not in PI4KIIα knockout MCF-7 cells, indicating that it is highly selective for PI4KIIα.  Importantly, PI-273 inhibited MCF-7 cell-induced breast tumor growth in mouse xenograft models without toxicity.

SMILE:  CC1=C(CC)C(C(N)=O)=C(NC(NC(C2=CC=C(Cl)C=C2)=O)=S)S1

Systematic Name:  2-(3-(4-chlorobenzoyl)thioureido)-4-ethyl-5-methylthiophene-3-carboxamide 

Molecular Weight:  381.89

Formula:  C16H16ClN3O2S2

PMID:  28827373