MK2-IN-5 acetate

MK2-IN-5 (Hsp25 kinase inhibitor) acetate is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 acetate targets the protein interaction domain in the MAPK pathway. MK2-IN-5 acetate inhibits HSP25 and HSP27 phosphorylation.

MK2-IN-5 acetate (5-10 μM, 2 h) inhibits TGF-b1 induced connective tissue growth factor (CTGF) and collagen type I in primary human keloid fibroblasts^[3].

MK2-IN-5 acetate (2 mg/kg Intraperitoneal injection, single dose) decreased HSP25 phosphorylation in ventilator-associated lung injury model^[2].

References:
[1]. Gaestel M, et al. Peptides as signaling inhibitors for mammalian MAP kinase cascades [J]. Current pharmaceutical design, 2009, 15(21): 2471-2480.
[2]. Damarla M, et al. Mitogen activated protein kinase activated protein kinase 2 regulates actin polymerization and vascular leak in ventilator associated lung injury [J]. PloS one, 2009, 4(2): e4600.
[3]. Lopes L B, et al. Inhibition of HSP27 phosphorylation by a cell-permeant MAPKAP Kinase 2 inhibitor [J]. Biochemical and biophysical research communications, 2009, 382(3): 535-539.