Description
YC-1 is a guanylyl cyclase activator and HIF-1α inhibitor. YC-1 displays anti-fibrotic, anticancer chemotherapeutic, anti-atherosclerotic, and neuroprotective activities. In vitro, YC-1 decreases secretion of sENG and sFlt-1, reversing endothelial dysfunction. In hepatic stellate cells, this compound decreases cell viability and increases apoptosis, potentially through suppressing expression of αSMA. In canine lymphoma cells, YC-1 inhibits cell proliferation; in similar animal models, it induces tumor regression. In other animal models, YC-1 decreases ox-LDL-induced cholesterol accumulation. Additionally, this compound suppresses neuronal death induced by amyloid-β (Aβ) peptides.
References
Brownfoot FC, Tong S, Hannan NJ, et al. YC-1 reduces placental sFlt-1 and soluble endoglin production and decreases endothelial dysfunction: A possible therapeutic for preeclampsia. Mol Cell Endocrinol. 2015 Sep 15;413:202-8. PMID: 26159901.
Xiao J, Jin C, Liu Z, et al. The design, synthesis, and biological evaluation of novel YC-1 derivatives as potent anti-hepatic fibrosis agents. Org Biomol Chem. 2015 Jul 14;13(26):7257-64. PMID: 26055070.
Kambayashi S, Igase M, Kobayashi K, et al. Hypoxia inducible factor 1α expression and effects of its inhibitors in canine lymphoma. J Vet Med Sci. 2015 Jun 6. [Epub ahead of print]. PMID: 26050843.
Tsou CY, Chen CY, Zhao JF, et al. Activation of soluble guanylyl cyclase prevents foam cell formation and atherosclerosis. Acta Physiol (Oxf). 2014 Apr;210(4):799-810. PMID: 24299003.
Purohit R, Fritz BG, The J, et al. YC-1 binding to the β subunit of soluble guanylyl cyclase overcomes allosteric inhibition by the α subunit. Biochemistry. 2014 Jan 14;53(1):101-14. PMID: 24328155.
Tsai YC, Lee YM, Lam KK, et al. The role of heat shock protein 70 in the protective effect of YC-1 on β-amyloid-induced toxicity in differentiated PC12 cells. PLoS One. 2013 Jul 26;8(7):e69320. PMID: 23922702.
