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Rocilinostat (also known as ACY 1215) is a selective HDAC6 inhibitor with potential antineoplastic activity. Rocilinostat (ACY-1215) selectively targets and binds to HDAC6, thereby disrupting the Hsp90 protein chaperone system through hyperacetylation of Hsp90 and preventing the subsequent aggresomal protein degradation. ACY-1215 has minimal activity (IC50 >1 μM) against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1 and Sirtuin2, and has slight activity against HDAC8 (IC50 = 0.1 μM). In vivo, the anti-MM activity of rocilinostat in combination with bortezomib was confirmed using 2 different xenograft SCID mouse models: human MM injected subcutaneously and luciferase-expressing human MM injected intravenously. Rocilinostat (ACY-1215) induces potent acetylation of α-tubulin at very low doses and triggers acetylation of lysine on histone H3 and histone H4 only at higher doses. Compared to non-selective HDAC inhibitor, ACY-1215 is able to reduce the toxic effects on normal, healthy cells.
| Molecular Weight | 433.5 |
| Formula | C24H27N5O3 |
| CAS Number | 1316214-52-4 |
| Solubility (25°C) | DMSO 77 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related HDAC Products |
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CM-444 is an inhibitor for HDAC and DNA methyltransferases (DNMT) with IC50 values of 6 nM-0.6 μM and 1.8-2.3 μM, respectively. CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models. |
| CM-1758
CM-1758 is a histone deacetylase (HDAC) inhibitor. CM-1758 inhibits tumor growth in vivo. CM-1758 induces acetylation of non-histone proteins in acute myeloid leukemia cells. |
| T-518
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| SE-7552
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| BRD9757
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