PIP4K-IN-a131

• CAT Number: I015456
• CAS Number: 2055405-95-1
• Molecular Formula: C20H13N3
• Molecular Weight: 295.34
• Purity: ≥95%
• Synonyms: (Z)-2-(1H-indol-3-yl)-3-isoquinolin-5-ylprop-2-enenitrile
• InChI: InChI=1S/C20H13N3/c21-11-16(19-13-23-20-7-2-1-6-18(19)20)10-14-4-3-5-15-12-22-9-8-17(14)15/h1-10,12-13,23H/b16-10+
• InChIKey: GWWKEWLUVHLNEX-MHWRWJLKSA-N
• SMILES: C1=CC=C2C(=C1)C(=CN2)C(=CC3=CC=CC4=C3C=CN=C4)C#N

PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC50s of 1.9 µM and 0.6 µM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways[1].
PIP4K-IN-a131 (0-100 μM; 72?hours) is a potent antiproliferative agent with a clear selectivity toward cancer cells killing[1].?
PIP4K-IN-a131 eliminates cancer cells via a dual-inhibitory mechanism[1].?
PIP4K-IN-a131 causes inhibition of the PI3K/Akt/mTOR pathway only in normal BJ cells, but not in transformed counterparts[1].?
Inhibition of PIP4Ks by PIP4K-IN-a131 arrests normal cells at the G1/S phase of the cell cycle by suppressing the PI3K/Akt/mTOR signaling pathway via transcriptional upregulation of PIK3IP1[1].

Reference

[1]. Mayumi Kitagawa, et al. Dual Blockade of the Lipid Kinase PIP4Ks and Mitotic Pathways Leads to Cancer-Selective Lethality. Nat Commun. 2017 Dec 19;8(1):2200.
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