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Rocilinostat (ACY-1215)

Cat No.
CEI-1509
Description
Rocilinostat (ACY-1215) is a selective inhibitor of HDAC6 with IC50 of 5 nM.
Product Overview
Rocilinostat (ACY-1215) is a selective inhibitor of HDAC6 with IC50 of 5 nM. HDAC6 (histone deacetylase 6) is an enzyme which encoded by the HDAC6 gene and plays an important role in translational regulation, cell cycle progression and developmental events. It has been revealed that over-expression of HDAC6 is correlated with tumorigenesis and cell survival and HDAC6 also involves in cancer cells metastasis. Rocilinostat (ACY-1215) is a selective HDAC6 inhibitor. When tested with human MM cell lines (MM. 1S), treatment with ACY-1215 in increasing dose for 6 hours increased acetylated α-tubulin at a concentration of 0.62μM via inhibiting HDAC6.In multiple myeloma cells, used ACY-125 as an adjuvant with carfilzomib triggered synergistic anti-MM effects, even in bortezomib-resistant cells which resulted in enhance cells apoptosis. In mouse model with xenografted human MM cells, administration of ACY-125 only or with bortezomib could markedly delay tumor growth and the combination showed best efficacy. It is also reported that ACY-1215 has minimal activity against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1, and Sirtuin2 (IC50 >1μM), and has slight activity against HDAC8 (IC50 = 0.1μM). When tested with mouse xenografted MM cells, combination carfilzomib with ACY-1215 showed a decreased effect on tumor volume and cells apoptosis.
CAS No.
1316214-52-4
Molecular Weight
433.5
Purity
0.9949
Storage
Store at -20°C
Targets
HDAC6
IC50
5 nM
Molecular Formula
C24H27N5O3
Chemical Name
N-[7-(hydroxyamino)-7-oxoheptyl]-2-(N-phenylanilino)pyrimidine-5-carboxamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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