delcasertib

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Ligands
delcasertib

GtoPdb Ligand ID: 7840

Synonyms: BMS-875944 | CS-9803 | KAI-9803

Compound class: Peptide or derivative

Comment: The synthesis of delcasertib is described in [1]. Delcasertib is a peptidic agent which is an isozyme-selective delta protein kinase C (PKCδ) inhibitor. It consists of a cargo peptide (CSFNSYELGSL) derived from the δV1-1 portion of PKCδ which acts to inhibit PKCδ translocation, conjugated to the cell-penetrating, arginine-rich peptide sequence of the HIV type 1 transactivator protein (TAT_45-57 CYGRKKRRQRRR) which acts as a cellular delivery system.

Summary
Biological activity
Clinical data
References
Structure

Bioactivity Comments
In cellular assays the δV1-1 peptide inhibits PMA-induced PKCδ translocation., but does not inhibit translocation of PKCε or PKCα, indicating PKCδ selectivity [1]. There appears to be no publicly available affinity data for this compound at PKCδ.

Bioactivity Comments

In cellular assays the δV1-1 peptide inhibits PMA-induced PKCδ translocation., but does not inhibit translocation of PKCε or PKCα, indicating PKCδ selectivity [1]. There appears to be no publicly available affinity data for this compound at PKCδ.