420116

JNK Inhibitor I, (L)-Form, Cell-Permeable

The JNK Inhibitor I, (L)-Form, Cell-Permeable controls the biological activity of JNK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): JNK Inhibitor I, (L)-Form, Cell-Permeable, c-Jun NH₂-terminal kinase, SAPK Inhibitor I, (L)-JNKI1, ( L)-HIV-TAT₄₈₋₅₇-PP-JBD₂₀, H-GRKKRRQRRRPPRPKRPTTLNLFPQVPRSQDT-NH₂
• Empirical Formula (Hill Notation): C₁₆₈H₂₉₃N₆₇O₄₂
• Molecular Weight: 3923.55
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: lyophilized solid
• potency: 1 μM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic)
• color: white
• solubility: water: 2 mg/mL
• shipped in: ambient
• storage temp.: −20°C

Description

General description

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-TAT_48-57 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-TAT_48-57 sequence as a carrier peptide and two proline residues as spacer. Inhibits IL-1β-induced c-jun and c-fos expression in insulin secreting βTC-3 cells and offers protection against apoptosis. Does not affect insulin secretion and has no effect on either ERK 1/2 or p38 activities.

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-TAT_48-57 sequence that imparts cell-permeability. Blocks the activation domain of c-Jun NH₂-terminal kinase (JNK) and prevents the activation of the transcription factor c-Jun (IC₅₀ ~1 µM). Contains the minimal 20-amino acid inhibitory domain of islet-brain (IB), which is critical for interaction with JNK.The peptide is covalently linked to the 10-amino acid HIV-TAT_48-57 sequence that acts as a carrier peptide and to two proline residue spacers. Inhibits IL-1β-induced c-Jun and c-fos expression in insulin secreting βTC-3 cells and offers protection against apoptosis. Does not affect insulin secretion and has no significant effect on the activities of ERK1, ERK2, or p38.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
JNK

Product does not compete with ATP.

Reversible: no

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Sequence

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

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Barr, R.K., et al. 2002. J. Biol. Chem.277, 10987.
Bonny, C., et al. 2001. Diabetes50, 77.

Legal Information

Sold under license of U.S. Patents 6,043,083 and 6,410,693.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable