Drug intelligence / Profile preview

CGK733

Development stage
Preclinical
Modality
Small Molecules
Administration
Laboratory/research Use Only; Not For Human Use
01

Overview

**CGK733** is a small-molecule inhibitor primarily reported to inhibit the serine/threonine kinases **ATM (atypical telangiectasia mutated)** and **ATR (ATM and Rad3-related)**, both of which are central regulators of the cellular response to DNA damage. By inhibiting these kinases (with IC50 values in the nanomolar range), CGK733 blocks DNA damage response (DDR) signaling, impairs double-stranded DNA break repair, and disrupts cell cycle checkpoints. It has been shown to sensitize cells to radiotherapy and genotoxic chemotherapeutic agents, enhance cytotoxicity in cancer models, and induce cell death in senescent and cancer cells. There is also evidence for neuroprotective effects through amelioration of acrylamide-induced toxicity, modulation of autophagy-related pathways, and inhibition of RANKL-induced signaling in osteoclast differentiation. There is controversy over the specificity and reproducibility of its reported activities, with some landmark studies retracted, but subsequent research generally supports its action as an ATM/ATR inhibitor[1][4][6][10]. CGK733 is used strictly for research and is not approved for human therapeutic use.

Other names
CGK 733CGK733CGK-733ATM/ATR Kinase Inhibitor
02

Targets

ATM (Ataxia telangiectasia mutated protein)

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