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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 (TAT45-57 CYGRKKRRQRRR) which acts as a cellular delivery system.
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Peptide Sequence  |
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| Cys(1)-Ser-Phe-Asn-Ser-Tyr-Glu-Leu-Gly-Ser-Leu-Cys(1)-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg | |
| Chemical Modification | |
| In this peptide CSFNSYELGSL is termed the 'cargo' peptide, whilst CYGRKKRRQRRR is termed the 'carrier' peptide. The latter is used to deliver the cargo peptide to its site of action. The two peptides are joined by a disulphide bridge between the two cysteine residues. Sequences were obtained from patent US7265092 [4]. | |
