Myosin Light Chain Kinase Inhibitor Peptide 18 - Calbiochem (C15-1303-839)

General description

A highly basic, cell-permable, nonapeptide that acts as a selective myosin light chain kinase (MLCK) inhibitor (IC₅₀ = 50 nM). Does not block calmodulin (CaM) or inhibit the kinase activities of Ca²⁺/calmodulin kinase II (CaMKII) or protein kinase A (PKA). Inhibition is competitive with respect to substrate (K_i = 52 nM). Displays mixed mode inhibition with respect to ATP.

A highly basic, cell-permeable, nonapeptide that acts as a selective Myosin Light Chain Kinase (MLCK) inhibitor (IC₅₀ = 50 nM). The inhibition is competitive with respect to the peptide substrate (K_i = 52 nM) and displays a mixed mode of inhibition with respect to ATP. Does not interfere with kinase activation by calmodulin (CaM), nor does it inhibit the activities of CaMKII and PKA.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Mlck

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 50 nM against MLCK

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Sequence

H-Arg-Lys-Lys-Tyr-Lys-Tyr-Arg-Arg-Lys-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

Zolotarevsky, Y., et al. 2002. Gastroenterology123, 163.
Lukas, T.J., et al. 1999. J. Med. Chem.42, 910.

Legal Information

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

Molecular Weight: 1324.62. Empirical Formula: C₆₀H₁₀₅N₂₃O₁₁. Quality Level: 100. Assay: ≥. 97% (HPLC). form: lyophilized solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, desiccated (hygroscopic). color: white. solubility: water: 1 . mg/mL, DMSO: 5 . mg/mL. shipped in: wet ice. storage temp.: −. 20°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 1. Flash Point(F): Not applicable. Flash Point(C): Not applicable.