Drug intelligence / Profile preview

RA190

Development stage
Preclinical
Lead developer
Johns Hopkins University
Modality
Small Molecules
Administration
Oral, Intraperitoneal, Topical
01

Overview

RA190 is a **bis-benzylidine piperidone small molecule** that acts as a **covalent and irreversible inhibitor** of the proteasomal ubiquitin receptor RPN13 (also known as ADRM1). It binds specifically to cysteine 88 of RPN13, blocking proteasome function and leading to the accumulation of polyubiquitinated proteins, induction of endoplasmic reticulum stress, unfolded protein response, and apoptosis in tumor cells. RA190 is effective in models of multiple myeloma, ovarian cancer, and HPV-positive cancers, including those resistant to bortezomib. It is bioavailable via oral, intraperitoneal, or topical administration in mice, and demonstrates favorable tissue distribution without detectable toxicity at therapeutic doses[1][2][3].

Other names
RPN13 InhibitorRPN-13 InhibitorRPN 13 InhibitorADRM1 InhibitorADRM-1 InhibitorADRM 1 InhibitorAdhesion Regulating Molecule 1 InhibitorARM1 InhibitorARM-1 InhibitorARM 1 InhibitorGP110 InhibitorGP-110 InhibitorGP 110 Inhibitor
02

Targets

PSMD13 (Proteasome 26S subunit non-ATPase 13)UCHL5 (Ubiquitin carboxyl-terminal hydrolase isozyme L5)

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