MC1568 interferes with myogenic signaling by blocking HDAC enzymatic activity and MEF2-mediated transactivation in C2C12 cells. Exposure of rat intestinal epithelial cell line EIC-18 to MC1568 prevented stimulation of DNA synthesis and blocked cell cycle progression in the G0/G1 phase. In a mice carotid ligation model, MC1568 has been shown to mediate proliferation and migration of smooth muscle cells in vitro, and thus may reduce blood pressure in hypertensive animals.
| Cas No. | 852475-26-4 |
|---|---|
| Purity | ≥98% |
| Formula | C17H15FN2O3 |
| Formula Wt. | 314.32 |
| Chemical Name | (2E)-3-{4-[(1E)-3-(3-Fluorophenyl)-3-oxo-1-propen-1-yl]-1-methyl-1H-pyrrol-2-yl}-N-hydroxyacrylamide |
| Solubility | 100mM in DMSO |
| Store Temp | -20°C |
|---|---|
| Ship Temp | Ambient |
| MSDS | |
|---|---|
| Info Sheet |
Nebbioso A, Manzo F, Miceli M, et al. Selective class II HDAC inhibitors impair myogenesis by modulating the stability and activity of HDAC-MEF2 complexes. EMBO Rep. 2009 Jul;10(7):776-782. PMID: 19498465.
Sinnett-Smith J, Ni Y, Wang J, et al. Protein kinase D1 mediates class IIa histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling. Am J Physiol Cell Physiol. 2014 May 15;306(10):C961-C971. PMID: 24647541.
Usui T, Morita T, Okada M, Yamawaki H. Histone deacetylase 4 controls neointimal hyperplasia via stimulating proliferation and migration of vascular smooth muscle cells. Hypertension. 2014 Feb;63(2):397-403. PMID: 24166750.
Lemon DD, Harrison BC, Horn TR, et al. Promiscuous actions of small molecule inhibitors of the protein kinase D-class IIa HDAC axis in striated muscle. FEBS Lett. 2015 Apr 28;589(10):1080-1088. PMID: 25816750.
