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Merck
CN

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

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About This Item

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)
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Quality Segment

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

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-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-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)


Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable



Certificates of Analysis (COA)

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Global Trade Item Number

SKUGTIN
420116-1MG04055977187946