Merck, SML3143-1MG, CIGB-300 trifluoroacetate

Biochem/physiol Actions
CIGB-300 (P15-Tat) is a substrate-competitive casein kinase 2 inhibitor (CK2, CKII) composed of a membrane-permeant HIV-1 Tat protein transduction domain sequence (a.a. 48-60) N-terminal to a disulfide-bridged cyclic substrate peptide that inhibits against CK2-mediated substrate HPV-16 E7 phosphorylation in vitro. CIGB-300 exhibits cytotoxic effect in various cancer cultures (IC50 from 20 to 182 μM) via apoptosis induction and effectively inhibits TC-1 tumor growth in mice in vivo (48 μmol/200 μL/mouse via daily intratumoral injection).
Substrate-competitive casein kinase 2 (CK2, CKII) inhibitor with anti-cancer efficacy in cultures and in vivo.