1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. Citarinostat

Citarinostat (ACY241) is a second generation potent, orally active and high-selective HDAC6 inhibitor with an IC50 of 2.6 nM (IC50s of 35 nM, 45 nM, 46 nM and 137 nM for HDAC1, HDAC2, HDAC3 and HDAC8, respectively). Citarinostat has anticancer effects.

For research use only. We do not sell to patients.

Citarinostat Chemical Structure

Citarinostat Chemical Structure

CAS No. : 1316215-12-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Citarinostat (ACY241) is a second generation potent, orally active and high-selective HDAC6 inhibitor with an IC50 of 2.6 nM (IC50s of 35 nM, 45 nM, 46 nM and 137 nM for HDAC1, HDAC2, HDAC3 and HDAC8, respectively). Citarinostat has anticancer effects[1].

IC50 & Target[1]

HDAC6

2.6 nM (IC50)

HDAC1

35 nM (IC50)

HDAC2

45 nM (IC50)

HDAC3

46 nM (IC50)

HDAC8

137 nM (IC50)

HDAC7

7300 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
BV-173 IC50
0.9 μM
Compound: Citarinostat
Anti-proliferative activity against human BV-173 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human BV-173 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
Fibroblast IC50
5.7 μM
Compound: 6
Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method
Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
Fibroblast IC50
5.7 μM
Compound: ACY-241
Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
Fibroblast IC50
5.74 μM
Compound: ACY-241
Cytotoxicity against human normal fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human normal fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
Fibroblast IC50
7.4 μM
Compound: 6
Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method
Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
Fibroblast IC50
7.4 μM
Compound: ACY-241
Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
Fibroblast IC50
7.44 μM
Compound: ACY-241
Cytotoxicity against primary pooled human fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against primary pooled human fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
HeLa IC50
7 μM
Compound: Citarinostat
Anti-proliferative activity against human HeLa cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human HeLa cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
HuT78 IC50
1.78 μM
Compound: ACY-241
Cytotoxicity against human Hut78 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human Hut78 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
HUVEC IC50
4.86 μM
Compound: ACY-241
Cytotoxicity against human HUVEC cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human HUVEC cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
HUVEC IC50
4.9 μM
Compound: 6
Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
HUVEC IC50
4.9 μM
Compound: ACY-241
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
Jurkat IC50
1.2 μM
Compound: Citarinostat
Anti-proliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
MM1.S IC50
1.52 μM
Compound: 6
Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
MM1.S IC50
1.6 μM
Compound: Citarinostat
Anti-proliferative activity against human MM1.S cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human MM1.S cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
MM1.S IC50
1.61 μM
Compound: ACY-241
Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
MOLM-13 IC50
13.5 μM
Compound: Citarinostat
Anti-proliferative activity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
MOLT-4 IC50
1.72 μM
Compound: ACY-241
Cytotoxicity against human MOLT-4 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MOLT-4 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
MV4-11 IC50
1.2 μM
Compound: Citarinostat
Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
MV4-11 IC50
1.24 μM
Compound: 6
Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
MV4-11 IC50
1.24 μM
Compound: ACY-241
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
MV4-11 IC50
1.34 μM
Compound: ACY-241
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
MV4-11 IC50
1.34 μM
Compound: ACY-241
Cytotoxicity against human MV4-11 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MV4-11 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
NSC IC50
4.35 μM
Compound: ACY-241
Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
OCI-AML-3 IC50
7.7 μM
Compound: Citarinostat
Anti-proliferative activity against human AML-3 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human AML-3 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
RPMI-8226 IC50
3.16 μM
Compound: 6
Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
RPMI-8226 IC50
6.5 μM
Compound: Citarinostat
Anti-proliferative activity against human RPMI-8226 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human RPMI-8226 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
Sf9 IC50
> 1 μM
Compound: Citarinostat
Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay
[PMID: 31938464]
Sf9 IC50
0.318 μM
Compound: Citarinostat
Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
[PMID: 31938464]
Sf9 IC50
2.6 nM
Compound: ACY-241
Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substrate a
Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substrate a
[PMID: 31414801]
Sf9 IC50
35 nM
Compound: ACY-241
Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substr
Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substr
[PMID: 31414801]
SU-DHL-1 IC50
4.56 μM
Compound: ACY-241
Cytotoxicity against human SU-DHL-1 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human SU-DHL-1 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
U-87MG ATCC IC50
9.1 μM
Compound: Citarinostat
Anti-proliferative activity against human U87G cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human U87G cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
In Vitro

Citarinostat (ACY241; 0-3 μM; 24 hours; A2780 cells) treatment with 300 nM results in increased hyperacetylation of α-tubulin, consistent with inhibition of the tubulin deacetylase HDAC6. In contrast, hyperacetylation of histone H3, a target of Class I HDACs, is only observed at doses above 1 μM. Low exposures of Citarinostat result in selective inhibition of HDAC6, while higher exposures lead to inhibition of Class I HDAC isozymes[1].
The single agent viability IC50 of Citarinostat (ACY241) ranged from 4.6-6.1 μM in A2780 and TOV-21G ovarian cancer and MDA-MD-231 breast cancer cells. Consistent with the viability assay, single agent Citarinostat modestly reduces proliferation at doses up to 3 μM without inducing apoptosis, while 10 μM of Citarinostat causes significant induction of apoptosis and completely suppresses proliferation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: A2780 cells
Concentration: 0 μM, 0.1 μM, 0.3 μM, 0.5μM, 1 μM, 3 μM
Incubation Time: 24 hours
Result: Resulted in increased hyperacetylation of α-tubulin, consistent with inhibition of the tubulin deacetylase HDAC6. In contrast, hyperacetylation of histone H3, a target of Class I HDACs, was only observed at doses above 1 μM.
In Vivo

Citarinostat (ACY241; 50 mg/kg; intraperitoneal injection; once daily for five days, followed by two days off; for 3 weeks; female athymic nude mice) significantly suppresses tumor growth in combination with NSC 125973[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nude mice (7-week-old) injected with TOV-21G cells[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; once daily for five days, followed by two days off; for 3 weeks
Result: Combination treatment with NSC 125973 resulted in significantly suppression of tumor growth.
Clinical Trial
Molecular Weight

467.95

Formula

C24H26ClN5O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN=C(N(C2=CC=CC=C2Cl)C3=CC=CC=C3)N=C1)NCCCCCCC(NO)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (64.11 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1370 mL 10.6849 mL 21.3698 mL
5 mM 0.4274 mL 2.1370 mL 4.2740 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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  • Dilution Calculator

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.30%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1370 mL 10.6849 mL 21.3698 mL 53.4245 mL
5 mM 0.4274 mL 2.1370 mL 4.2740 mL 10.6849 mL
10 mM 0.2137 mL 1.0685 mL 2.1370 mL 5.3425 mL
15 mM 0.1425 mL 0.7123 mL 1.4247 mL 3.5616 mL
20 mM 0.1068 mL 0.5342 mL 1.0685 mL 2.6712 mL
25 mM 0.0855 mL 0.4274 mL 0.8548 mL 2.1370 mL
30 mM 0.0712 mL 0.3562 mL 0.7123 mL 1.7808 mL
40 mM 0.0534 mL 0.2671 mL 0.5342 mL 1.3356 mL
50 mM 0.0427 mL 0.2137 mL 0.4274 mL 1.0685 mL
60 mM 0.0356 mL 0.1781 mL 0.3562 mL 0.8904 mL
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Product Name:
Citarinostat
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HY-15994
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