Drug intelligence / Profile preview

NSC-663284

Development stage
Preclinical
Lead developer
University of Pittsburgh
Modality
Small Molecules
01

Overview

NSC‑663284 is a potent, cell-permeable small molecule inhibitor of the Cdc25 family of dual specificity phosphatases (Cdc25A, Cdc25B, and Cdc25C). It acts by irreversibly inhibiting these phosphatases with nanomolar affinity (Ki values: 29 nM for Cdc25A; 95 nM for Cdc25B2; 89 nM for Cdc25C), showing high selectivity over other phosphatases such as VHR and PTP1B. By blocking the activity of these enzymes, NSC‑663284 arrests cells at both G1 and G2/M phases of the cell cycle through inhibition of cyclin-dependent kinase activation (cdk1/cdk2), leading to anti-proliferative effects in various human tumor cell lines. The compound is a quinolinedione derivative and has been studied primarily as an experimental anticancer agent in preclinical models[1][2][4][5][6].

Other names
6-chloro-7-(2-morpholinyl)ethylamino)quinoline-5,8-dione6-chloro-7-(2-morpholinoethyl)amino)quinoline-5,8-dioneCDC25 Phosphatase Inhibitor IICDC-25 Phosphatase Inhibitor IICDC 25 Phosphatase Inhibitor IIPTP Inhibitor XXIVHR Inhibitor II
02

Targets

CDC25A (Cell division cycle 25A phosphatase)CDC25B (Cell division cycle 25B phosphatase)CDC25C (Cell division cycle 25C phosphatase)

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