Drug intelligence / Profile preview

VS-II-173

Development stage
Preclinical
Lead developer
University of Caen Normandy
Modality
Small Molecules
01

Overview

VS-II-173 is a small molecule inhibitor of the Pim-1 kinase, characterized by a pyrazolo[4,3-a]phenanthridine scaffold. Developed by researchers at the University of Caen Normandy (CERMN), it is an antineoplastic agent specifically investigated for the treatment of acute myeloid leukemia (AML). Pim-1 is a serine/threonine kinase that promotes cell survival and proliferation; its overexpression is a hallmark of several hematological malignancies and is associated with resistance to chemotherapy. VS-II-173 acts as an ATP-competitive inhibitor, binding to the orthosteric site of the Pim-1 kinase to block its signaling pathways, thereby inducing apoptosis and inhibiting the growth of AML cells such as the MOLM-13 line. It has served as a structural template for the synthesis of subsequent generations of Pim inhibitors.

02

Targets

PIM1 (Proviral integration site for moloney murine leukemia virus kinase 1)AMP-activated protein kinase alpha-2/beta-1/gamma-1AMP-activated protein kinase alpha-2 beta-2 gamma-1AMP-activated protein kinase alpha-1/beta-2/gamma-1PIM3 (Proviral integration site for Moloney murine leukemia virus kinase 3)

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