Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 50 nM against MLCK

Primary TargetMlck

Cell permeable: yes

General description

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.

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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

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.

Sequence

H-Arg-Lys-Lys-Tyr-Lys-Tyr-Arg-Arg-Lys-NH₂

Warning

Toxicity: Standard Handling (A)