Home Epigenetics HDAC inhibitor Citarinostat (ACY-241) For research use only.

Citarinostat (ACY-241)

Synonyms: HDAC-IN-2

Citarinostat (ACY-241, HDAC-IN-2) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3.

Citarinostat (ACY-241) Chemical Structure

Citarinostat (ACY-241) Chemical Structure

CAS No. 1316215-12-9

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Citarinostat (ACY-241) Related Products

Signaling Pathway

HDAC Signaling Pathways

HDAC Signaling Pathway

Biological Activity

Description Citarinostat (ACY-241, HDAC-IN-2) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3.
Targets
HDAC6 [1]
(Cell-free assay)		 HDAC1 [1]
(Cell-free assay)		 HDAC2 [1]
(Cell-free assay)		 HDAC3 [1]
(Cell-free assay)		 HDAC8 [1]
(Cell-free assay)
2.6 nM 35 nM 45 nM 46 nM 137 nM
In vitro
In vitro

In cell lines from multiple solid tumor lineages, combination treatment with ACY-241 enhances inhibition of proliferation and increases cell death relative to either single agent alone. Combination treatment with ACY-241 also results in more frequent occurrence of mitotic cells with abnormal multipolar spindles and aberrant mitoses, and is associated with increased frequency of abnormal multipolar mitotic spindle formation, induction of aneuploidy, and increased cell death. In A2780 ovarian cancer cells, 24 hour treatment with 300 nM ACY-241 results in increased hyperacetylation of α-tubulin, consistent with inhibition of the tubulin deacetylase HDAC6. Low exposures of ACY-241 result in selective inhibition of HDAC6, while higher exposures lead to inhibition of Class I HDAC isozymes[1].
Cell Research Cell lines A2780 ovarian cancer cells
Concentrations 0.1, 0.3, 0.5, 1, 3 μM
Incubation Time 24 h
Method

A2780 cells are cultured with vehicle or a range of ACY-241 concentrations for 24 hours prior to immunoblotting.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Ac-Tubulin / Ac-H3K56 Ac-H3K9 Cell viability 27926524
In Vivo
In vivo

ACY-241 has a favourable safety profile than non-selective pan-HDAC inhibitors. It has the potential for a substantially reduced side effect profile versus current nonselective HDAC inhibitor drug candidates due to reduced potency against Class I HDACs while retaining the potential for anticancer effectiveness[1].
Animal Research Animal Models Female athymic nude mice (Crl:NU(NCr)-Foxn1nu)
Dosages 50 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02935790 Completed
Malignant Melanoma
Celgene|Syneos Health|ApoCell Inc.|Celerion|NYU Langone Health
 September 30 2016 Phase 1
NCT02635061 Terminated
Non Small Cell Lung Cancer
Celgene
 August 25 2016 Phase 1
NCT02551185 Completed
Advanced Solid Tumors
Celgene
 December 22 2015 Phase 1
NCT02400242 Active not recruiting
Multiple Myeloma
Celgene
 May 7 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 467.95 Formula

C24H26ClN5O3
CAS No. 1316215-12-9 SDF Download Citarinostat (ACY-241) SDF
Smiles C1=CC=C(C=C1)N(C2=CC=CC=C2Cl)C3=NC=C(C=N3)C(=O)NCCCCCCC(=O)NO
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 93 mg/mL

DMSO : 41 mg/mL ( (87.61 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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