(±)-CPSI-1306

(±)-CPSI-1306 is an orally available antagonist of macrophage migration inhibitory factor (MIF).

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

Research Areas >> Metabolic Disease

MIF[1].

Mice treated with CPSI-1306 show a significant drop in their blood glucose levels, which is associated with a reduction in serum levels of inflammatory cytokines. As expected, control mice treated with vehicle develop NIDDM as characterized by high serum levels of glucose and inflammatory cytokine. Furthermore, they also show that orally bioavailable CPSI-1306 can be effective in treating this disease[1]. CPSI-1306-induced keratinocyte apoptosis could be appreciated as early as 30 minutes after a single UVB exposure. At 6, 24, and 48 hours following UVB exposure, the CPSI-1306-treated mice show significantly increased expression of cleaved caspase-3 compared with the vehicle-treated mice. CPSI-1306 reduces acute UVB-induced keratinocyte DNA damage and UVB-induced acute inflammation[2].

Mice[1] Six- to 8-wk-old female BALB/c mice and ICR mice are used in the study. Age- and sex-matched ICR mice are deprived of food for 20 h and then injected intraperitoneally with STZ (90 mg/kg). Beginning at 6 h after STZ injection, mice are administered CPSI-1306 (1 or 0.1 mg/kg) or PBS daily in a single oral dose for 30 d[1].

[1]. Sanchez-Zamora Y, et al. Macrophage migration inhibitory factor is a therapeutic target in treatment of non-insulin-dependent diabetes mellitus. FASEB J. 2010 Jul;24(7):2583-90.

[2]. Nagarajan P, et al. MIF antagonist (CPSI-1306) protects against UVB-induced squamous cell carcinoma. Mol Cancer Res. 2014 Sep;12(9):1292-302.

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