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βRepZnC
- Development stage
- Preclinical
- Lead developer
- Stanford University
- Modality
- Small Molecules
01
Overview
βRepZnC is a zinc-chelating hybrid small molecule designed for targeted pancreatic β-cell regeneration in the treatment of diabetes. It is a derivative of GNF-4877, a known replication-promoting compound that acts as a DYRK1A inhibitor. βRepZnC is engineered to leverage the uniquely high endogenous zinc concentrations found within the insulin granules of pancreatic β-cells. By incorporating a zinc-chelating moiety, the drug achieves cell-specific accumulation and retention, thereby restricting its bioactivity to β-cells and reducing potential off-target effects in other tissues. Research presented at ADA 2025 indicates that its delivery and regenerative efficacy can be significantly enhanced by co-administration with agents like GR-46611, which increase β-cell zinc flux through V-ATPase-driven granule acidification.
- Other names
- zinc-chelating hybrid compound of GNF-4877betaRepZnC
02
Targets
DYRK1A (Dual-specificity tyrosine-phosphorylation-regulated kinase 1A)
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