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Citarinostat

Catalog No. T3661 CAS 1316215-12-9

Synonyms: ACY241, HDAC-IN-2

ACY-241, also known as Citarinostat (ACY241), is a potent, selective and orally available histone deacetylase (HDAC) inhibitor, with potential antineoplastic activity. Upon oral administration, ACY-241 inhibits the activity of HDACs; this results in an accumulation of highly acetylated chromatin histones, the induction of chromatin remodeling and an altered pattern of gene expression. This leads to the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes, which inhibit tumor cell division and induce tumor cell apoptosis.

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Citarinostat, CAS 1316215-12-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 44.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 222.00
50 mg	In stock	$ 372.00
100 mg	In stock	$ 538.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 98.95%

Purity: 98.54%

Biological Description

Chemical Properties

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Description	ACY-241, also known as Citarinostat (ACY241), is a potent, selective and orally available histone deacetylase (HDAC) inhibitor, with potential antineoplastic activity. Upon oral administration, ACY-241 inhibits the activity of HDACs; this results in an accumulation of highly acetylated chromatin histones, the induction of chromatin remodeling and an altered pattern of gene expression. This leads to the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes, which inhibit tumor cell division and induce tumor cell apoptosis.
Targets&IC50	HDAC6:2.6 nM, HDAC8:137 nM, HDAC1:35 nM, HDAC3:46 nM, HDAC2:45 nM
In vitro	In cell lines from multiple solid tumor lineages, combination treatment with ACY-241 and paclitaxel enhances inhibition of proliferation and increases cell death relative to either single agent alone. Combination treatment with ACY-241 and paclitaxel 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].
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].
Cell Research	A2780 cells are cultured with vehicle or a range of ACY-241 concentrations for 24 hours prior to immunoblotting.(Only for Reference)

Synonyms	ACY241, HDAC-IN-2
Molecular Weight	467.95
Formula	C24H26ClN5O3
CAS No.	1316215-12-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 37 mg/mL(79.1 mM)

References and Literature

1. Huang P, et al. Oncotarget. 2017, 8(2):2694-2707.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Cancer Cell Differentiation Compound Library DNA Damage & Repair Compound Library Target-Focused Phenotypic Screening Library Anti-Aging Compound Library Epigenetics Compound Library

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Tenovin-6 Hydrochloride Oxamflatin Belinostat RTS-V5 CDK/HDAC-IN-3 HDAC-IN-4 HDAC ligand-1 CXD101

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Keywords

Citarinostat 1316215-12-9 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Histone deacetylases inhibit combination anticancer ACY 241 ACY-241 ACY241 HDAC6 Inhibitor anti-proliferation α-tubulin multiple. myeloma HDAC-IN-2 inhibitor

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