Drug intelligence / Profile preview

CAY10603

Development stage
Preclinical
Lead developer
Cayman Chemical
Modality
Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intraperitoneal (preclinical Studies)
01

Overview

CAY10603 is a potent and highly selective small molecule inhibitor of histone deacetylase 6 (HDAC6), with an IC50 of 2 pM and over 200-fold selectivity compared to other HDAC isoforms. It acts by targeting the active site zinc ion in HDAC6, thereby inhibiting its deacetylase activity. This inhibition affects both histone and non-histone proteins such as tubulin, impacting microtubule stability and cellular processes related to cancer cell proliferation and survival. Preclinical studies have shown that CAY10603 can suppress the growth of several pancreatic cancer cell lines and demonstrates protective effects in models of acute kidney injury (AKI) and chronic kidney disease (CKD). Additionally, it has been investigated for its potential to enhance radiotherapy efficacy in meningioma brain tumors by increasing tumor cell death when combined with radiation[1][2][4][7][9][10].

Other names
N-[4-[3-[[[7-(hydroxyamino)-7-oxoheptyl]amino]carbonyl]-5-isoxazolyl]phenyl]-carbamic acid 1,1-dimethylethyl esterHistone Deacetylase Inhibitor VIII
02

Targets

HDAC6 (Histone deacetylase 6)

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