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-TAT_48-57-PP-JBD₂₀, H-GRKKRRQRRRPPRPKRPTTLNLFPQVPRSQDT-NH₂
• Empirical Formula (Hill Notation): C₁₆₈H₂₉₃N₆₇O₄₂
• Molecular Weight: 3923.55
• NACRES: NA.77
• UNSPSC Code: 12352200
• Assay: ≥97% (HPLC)
• Form: lyophilized solid
• Storage condition: OK to freeze, desiccated (hygroscopic)

Properties

• Quality Segment: 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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
JNK

Product does not compete with ATP.

Reversible: no

Packaging

Packaged under inert gas

Physical form

Supplied as a trifluoroacetate salt.

Preparation Note

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.

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

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

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable