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| Cat. Number | M2409 |
| Chemical Name | M2409 MGCD-0103 726169-73-9 |
| CAS Number | 726169-73-9 |
| Mol. Formula | C23H20N6O |
| Mol. Weight | 396.44 |
| Qty 1 |
5mg |
| Qty 2 | 50mg |
| Appearance | Off white powder |
| Application Notes | ≥98% |
| Synonym | Mocetinostat |
| Solubility | DMSO 13 mg/mL (32.79 mM) Water Insoluble Ethanol Insoluble |
| Storage condition | -20°C |
| References | MGCD-0103 (Mocetinostat) is a benzamide histone deacetylase (HDAC) inhibitor that exhibits anticancer chemotherapeutic, anti-fibrotic, antihypertensive, and cardiomodulatory activities. MGCD-0103 is currently in clinical trials as a potential treatment for several leukemias and lymphomas. In sham hearts, MGCD-0103 improves left ventricular and end diastolic pressure and decreases total collagen levels; in CD90+ cells, it decreases levels of collagen III, matrix metalloproteinase 2, and α-SMA. In other models, MGCD-0103 increases natriuretic peptide receptor (NPR1) promoter activity, increasing transcription of guanyl cyclase A/natriuretic peptide receptor A. MGCD-0103 also decreases pulmonary artery pressure, right ventricular hypertrophy, and vascular remodeling in animal models of myocardial infarction and heart failure. Additionally, this compound induces apoptosis, activates PI3K/Akt/mTOR signaling, and decreases autophagy in chronic lymphocytic leukemia (CLL) cells. ReferencesNural-Guvener HF, Zakharova L, Nimlos J, et al. HDAC class I inhibitor, Mocetinostat, reverses cardiac fibrosis in heart failure and diminishes CD90+ cardiac myofibroblast activation. Fibrogenesis Tissue Repair. 2014 Jul 2;7:10. PMID: 25024745. Kumar P, Tripathi S, Pandey KN. Histone deacetylase inhibitors modulate the transcriptional regulation of guanylyl cyclase/natriuretic peptide receptor-a gene: interactive roles of modified histones, histone acetyltransferase, p300, AND Sp1. J Biol Chem. 2014 Mar 7;289(10):6991-7002. PMID: 24451378. El-Khoury V, Pierson S, Szwarcbart E, et al. Disruption of autophagy by the histone deacetylase inhibitor MGCD0103 and its therapeutic implication in B-cell chronic lymphocytic leukemia. Leukemia. 2014 Aug;28(8):1636-46. PMID: 24418989. Cavasin MA, Demos-Davies K, Horn TR, et al. Selective class I histone deacetylase inhibition suppresses hypoxia-induced cardiopulmonary remodeling through an antiproliferative mechanism. Circ Res. 2012 Mar 2;110(5):739-48. PMID: 22282194. Younes A, Oki Y, Bociek RG, et al. Mocetinostat for relapsed classical Hodgkin's lymphoma: an open-label, single-arm, phase 2 trial. Lancet Oncol. 2011 Dec;12(13):1222-8. PMID: 22033282. |
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