MMI-0100 is a cell-penetrable peptide inhibitor of mitogen-activated protein kinase-activated protein kinase II (MK2). MMI-0100 reduces intimal hyperplasia in vitro & in vivo. MMI-0100 inhibits IL-6 expression without affecting IL-8 expression. MMI-0100 inhibits fibrotic processes like vein graft disease.
MMI-0100 is a cell-permeant peptide inhibitor of mitogen-activated protein kinase-activated protein kinase II (MK2, also known as MAPKAPK2). It effectively reduces intimal hyperplasia ex vivo and in vivo, suppresses IL-6 expression without affecting IL-8, and inhibits fibrotic processes such as vein graft disease. It has potential applications in cardiovascular and fibrotic diseases. Target: MK2/MAPKAPK2 (mitogen-activated protein kinase-activated protein kinase 2). MMI-0100 is a cell-permeant peptide that binds to MK2, inhibiting its kinase activity. MK2 is downstream of p38 MAPK and regulates post-transcriptional control of inflammatory mediators (TNF-alpha, IL-6) through AU-rich element (ARE)-mediated mRNA stability. MK2 inhibition suppresses inflammation and fibrosis. In vitro, in cultured vascular smooth muscle cells (VSMCs) and fibroblasts, MMI-0100 (1-50 uM) suppresses IL-6 expression without affecting IL-8. It inhibits MK2 autophosphorylation and reduces phosphorylation of HSP27, a downstream MK2 substrate. In VSMCs, MMI-0100 reduces proliferation and migration. In in vitro fibrosis models, it suppresses collagen synthesis and myofibroblast differentiation. In vivo, in rodent models of intimal hyperplasia (carotid artery balloon injury or vein graft models), systemic administration of MMI-0100 significantly reduces neointima formation and vessel wall thickening. In myocardial infarction models, MMI-0100 inhibits cardiac fibrosis and preserves cardiac function. For cell-free MK2 kinase inhibition assay: recombinant MK2 (10 ng) is incubated with varying concentrations of MMI-0100 (0-100 uM) and a peptide substrate (e.g., KKRPKRATSNVFS-NH2 or HSP27-derived peptide) in the presence of 33P-ATP in kinase buffer for 30 min at 30degC. Reactions are spotted onto P81 filter paper, washed, and radioactivity counted. IC50 is calculated. For cell assays: VSMCs or fibroblasts are serum-starved overnight, pretreated with MMI-0100 (1-50 uM) for 1 h, then stimulated with LPS (1 ug/mL) or TNF-alpha (10 ng/mL) for 4-24 h. Supernatant IL-6 is measured by ELISA. Cell lysates are analyzed by Western blot for p-MK2 (Thr334), p-HSP27 (Ser82), and MK2 expression. For in vivo animal studies: in rat carotid artery balloon injury model, rats undergo balloon injury of the common carotid artery. MMI-0100 is administered via intraperitoneal injection (10-30 mg/kg daily) or perivascular gel application for 14 days. Arteries are harvested, sectioned, and stained with hematoxylin and eosin and Verhoeff‘s elastin stain. Intimal and medial areas are measured to calculate intima-to-media ratio. PK properties of MMI-0100: As a peptide (MW 2283.64 Da), MMI-0100 is not orally bioavailable. It is administered by injection (IP, IV, SC) or local application. In rats, half-life is short (30-60 min) due to proteolytic degradation. Plasma clearance is rapid; tissue distribution favors vascular tissues. No toxicity data have been specifically reported. As an MK2 inhibitor that suppresses IL-6, immune function may be modulated, potentially increasing infection risk. No acute toxicity observed at therapeutic doses in rat studies (up to 30 mg/kg IP). MMI-0100 is a research compound not approved for clinical use. It is being developed for preventing vein graft failure and restenosis after angioplasty, as well as for treating cardiac fibrosis after myocardial infarction. It serves as a tool for studying MK2 biology in inflammation, fibrosis, and cardiovascular diseases.

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.