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BDP5290
- Development stage
- Preclinical
- Lead developer
- Beatson Institute
- Modality
- Small Molecules
- Administration
- Oral, Topical, Subcutaneous, Intravenous, Intramuscular, Inhalation, Intranasal, Rectal, Sublingual, Buccal, Transdermal, Intradermal, Intrathecal, Intraarticular, Intralesional, Intraperitoneal, Intra-arterial, Parenteral
01
Overview
BDP5290 (also known as BDP00005290) is a potent, selective small-molecule inhibitor of myotonic dystrophy kinase-related Cdc42-binding kinases (MRCK), specifically targeting MRCKα (CDC42BPA) and MRCKβ (CDC42BPB). Developed by the Cancer Research UK Beatson Institute, BDP5290 acts by binding to the nucleotide-binding pocket of the MRCK kinase domain, thereby blocking the phosphorylation of myosin light chain (MLC). This inhibition disrupts actin-myosin contractility, leading to the reduction of cancer cell motility, migration, and invasion. BDP5290 has been investigated in preclinical research for its potential to overcome immunotherapy resistance and suppress metastasis in various cancers, including breast cancer, colorectal cancer, and squamous cell carcinoma.
- Other names
- 4-chloro-1-(4-piperidyl)-N-[5-(2-pyridyl)-1H-pyrazol-4-yl]pyrazole-3-carboxamide
02
Targets
ROCK1 (Rho-associated coiled-coil containing protein kinase 1)ROCK2 (Rho-associated coiled-coil containing protein kinase 2)CDC42BPA (CDC42 binding protein kinase alpha)CDC42BPB (MRCKβ)
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