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
Quality Level
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 (Ki = 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 (Ki = 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
Mlck
Product does not compete with ATP.
Reversible: no
Target IC50: 50 nM against MLCK
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
H-Arg-Lys-Lys-Tyr-Lys-Tyr-Arg-Arg-Lys-NH₂
Zolotarevsky, Y., et al. 2002. Gastroenterology123, 163.
Lukas, T.J., et al. 1999. J. Med. Chem.42, 910.
Lukas, T.J., et al. 1999. J. Med. Chem.42, 910.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Nicholas J Hunt et al.
The journals of gerontology. Series A, Biological sciences and medical sciences, 75(2), 278-285 (2019-06-15)
Age-related changes in the liver sinusoidal endothelium, particularly the reduction in fenestrations, contribute to insulin resistance in old age. Metformin impacts on the aging process and improves insulin resistance. Therefore, the effects of metformin on the liver sinusoidal endothelium were
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