Drug intelligence / Profile preview

y-33075

Development stage
Preclinical
Lead developer
Sumitomo Pharma
Modality
Small Molecules
Administration
Not Established (preclinical Studies: Cellular/ex Vivo Administration)
01

Overview

**Y-33075** is a synthetic small molecule and non-selective inhibitor of Rho-associated coiled-coil containing protein kinase (ROCK), targeting both ROCK1 and ROCK2 isoforms. The compound is structurally related to Y-27632 but displays approximately 10-fold higher potency for inhibiting contraction in hepatic stellate cells (HSCs). Mechanistically, Y-33075 blocks ROCK-mediated phosphorylation of myosin light chain (MLC), thereby inhibiting stress fiber assembly, cellular contraction, and fibrogenesis. It also shows marked neuroprotective and anti-inflammatory effects by preserving retinal ganglion cell (RGC) viability and reducing microglial activation and gliosis. The drug has demonstrated promise in preclinical studies for conditions such as chronic liver disease/fibrosis and glaucoma, due to its dual action on both contraction/fibrogenesis and neuroprotection[1][3]. Molecular Formula: C16H16N4O; CAS Number: 199433-58-4[2].

Other names
4-[(1R)-1-aminoethyl]-N-1H-pyrrolo[2,3-b]pyridin-4-yl]benzamide
02

Targets

ROCK1 (Rho-associated coiled-coil containing protein kinase 1)PRKCI (Protein kinase C iota)ROCK2 (Rho-associated coiled-coil containing protein kinase 2)

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