Drug intelligence / Profile preview

IOR-160

Development stage
Preclinical
Lead developer
Institute of Oncology and Radiobiology
Modality
Small Molecules
01

Overview

IOR-160 is a small molecule dual inhibitor of Casein Kinase 2 (CK2) and Histone Deacetylase (HDAC) enzymes. Identified as a potent antitumor agent, it exhibits high selectivity for CK2 and broad inhibitory activity against HDAC isoforms 1, 2, 3, and 6. In preclinical models of triple-negative breast cancer (TNBC), IOR-160 has demonstrated the ability to significantly reduce tumor growth and burden without detectable toxicity. Its mechanism of action involves the modulation of critical cellular signaling pathways, specifically the inhibition of AKT phosphorylation and the induction of α-tubulin acetylation. Structural studies indicate that its binding mode to CK2 is highly conserved compared to the known CK2 inhibitor CX-4945.

02

Targets

CLK2 (CDC-like kinase 2)CK2 (Casein kinase II subunit alpha)DYRK1A (Dual-specificity tyrosine-phosphorylation-regulated kinase 1A)HDAC1 (Histone Deacetylase 1)HDAC2 (Histone deacetylase 2)HDAC3 (Histone Deacetylase 3)HDAC6 (Histone deacetylase 6)HDAC8 (Histone Deacetylase 8)HIPK2 (Homeodomain-interacting protein kinase 2)

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