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Rocilinostat (ACY-1215)Selective HDAC6 inhibitor

Rocilinostat (ACY-1215)

Catalog No. A4083
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $70.00 In stock
10mg $90.00 In stock
50mg $250.00 In stock
200mg $850.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1.Sun, Yuefeng, et al. "Fe65 Suppresses Breast Cancer Cell Migration and Invasion through Tip60 Mediated Cortactin Acetylation." Scientific reports 5 (2015). PMID:26166158

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Chemical structure

Rocilinostat (ACY-1215)

Related Biological Data

Rocilinostat (ACY-1215)

Related Biological Data

Rocilinostat (ACY-1215)

Related Biological Data

Rocilinostat (ACY-1215)

Biological Activity

Description Rocilinostat (ACY-1215) is a selective inhibitor of HDAC6 with IC50 of 5 nM.
Targets HDAC6          
IC50 5 nM          

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Chemical Properties

Cas No. 1316214-52-4 SDF Download SDF
Chemical Name N-[7-(hydroxyamino)-7-oxoheptyl]-2-(N-phenylanilino)pyrimidine-5-carboxamide
Canonical SMILES C1=CC=C(C=C1)N(C2=CC=CC=C2)C3=NC=C(C=N3)C(=O)NCCCCCCC(=O)NO
Formula C24H27N5O3 M.Wt 433.5
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Background

Rocilinostat (ACY-1215) is a selective inhibitor of HDAC6 with IC50 of 5 nM [1].
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 [2] [3].
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 [1]. 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 [2].
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 [1].
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) [1]. When tested with mouse xenografted MM cells, combination carfilzomib with ACY-1215 showed a decreased effect on tumor volume and cells apoptosis [2].
References:
[1].    Santo, L., et al., Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. Blood, 2012. 119(11): p. 2579-89.
[2].    Mishima, Y., et al., Ricolinostat (ACY-1215) induced inhibition of aggresome formation accelerates carfilzomib-induced multiple myeloma cell death. Br J Haematol, 2015.
[3].    Haakenson, J., et al., HDAC6-Dependent Functions in Tumor Cells: Crossroad with the MAPK Pathways. Crit Rev Oncog, 2015. 20(1-2): p. 65-81.