(L)-HIV-TAT48-57-PP-JBD20 (L)-JNKI1 c-Jun NH2-terminal kinase H-GRKKRRQRRRPPRPKRPTTLNLFPQVPRSQDT-NH2 SAPK Inhibitor I White lyophilized solid. Supplied as a trifluoroacetate salt. HYGROSCOPIC. PACKAGED UNDER INERT GAS. A cell-permeable, biologically active peptide consisting of a carboxyl terminal sequence derived from the JNK-binding domain (JBD) and an amino terminal peptide containing the HIV-TAT48-57 sequence. Blocks c-Jun NH2-terminal kinase (JNK) signaling by preventing the activation of the transcription factor c-jun (IC50 ~ 1 µM). This effect appears to be due to inhibition of phosphorylation of the activation domains of JNK. Contains the minimal 20-amino acid inhibitory domain of islet-brain (IB) that is shown to be critical for interaction with JNK linked to the 10-amino acid HIV-TAT48-57 sequence as a carrier peptide and two proline residues as spacer. Inhibits IL-1b-induced c-jun and c-fos expression in insulin secreting bTC-3 cells and offers protection against apoptosis. Does not affect insulin secretion and has no effect on either ERK 1/2 or p38 activities. Purity: ≥97% by HPLC. H-Gly-Arg-Lys-Lys-Arg-Agr-Gln-Arg-Arg-Arg-Pro-Pro-Arg-Pro-Lys-Arg-Pro-Thr-Thr-Leu-Asn-Leu-Phe-Pro-Gln-Val-Pro-Arg-Ser-Gln-Asp-Thr-NH2 Ref.: Barr, R.K., et al. 2002. J. Biol. Chem. 277, 10987. Bonny, C., et al. 2001. Diabetes 50, 77. Sold under license of U.S. Patents 6,043,083 and 6,410,693. |