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Drug intelligence / Profile preview
RGB-286147
- Development stage
- Preclinical
- Lead developer
- GPC Biotech
- Modality
- Small Molecules
- Administration
- Parenteral
01
Overview
RGB-286147 is a small-molecule, ATP-competitive inhibitor of cyclin-dependent kinases (CDKs) and CDK-related kinases (CRKs). Developed by GPC Biotech, it acts as a proteome-wide CDK/CRK inhibitor, targeting CDK1, CDK2, CDK3, CDK5, CDK7, CDK9, and atypical CDKs such as CDK14 (PFTK1), CDK16 (PCTK1), CDK18 (PCTK3), and CDK20 (CCRK). RGB-286147 exhibits potent cytotoxic activity against both cycling and non-cycling tumor cells, inducing cell cycle arrest in the G1 phase, inhibiting DNA replication, and triggering apoptosis. It has been investigated in preclinical research for its anti-tumor properties and as a tool to study molecular determinants of cancer cell survival.
- Other names
- Cdk7 Inhibitor IVCdk-7 Inhibitor IVCdk 7 Inhibitor IVCyclin-dependent kinase 7 Inhibitor IVCyclin-dependent kinase/CDK-related kinase Inhibitor
02
Targets
CDK20CDK16C-TAK1 (Cdc25C-associated kinase 1)CDK7CDK9 (Cyclin-dependent kinase 9)GSK3 (Glycogen synthase kinase 3 beta)CDK1 (Cyclin-dependent kinase 1)CDK2 (Cyclin-dependent kinase 2)CDK3 (Cyclin-dependent kinase 3)CDK5 (Cyclin-dependent kinase 5)CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)
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