1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. ACY-775

ACY-775 

Cat. No.: HY-19328 Purity: 99.54%
Handling Instructions

ACY-775 is a potent and selective inhibitor of the of histone deacetylase 6 (HDAC6) with an IC50 of 7.5 nM.

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

ACY-775 Chemical Structure

ACY-775 Chemical Structure

CAS No. : 1375466-18-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 196 In-stock
Estimated Time of Arrival: December 31
2 mg USD 108 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
25 mg USD 348 In-stock
Estimated Time of Arrival: December 31
50 mg USD 588 In-stock
Estimated Time of Arrival: December 31
100 mg USD 828 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

ACY-775 is a potent and selective inhibitor of the of histone deacetylase 6 (HDAC6) with an IC50 of 7.5 nM.

IC50 & Target[2]

HDAC6

7.5 nM (IC50)

HDAC1

2123 nM (IC50)

HDAC2

2570 nM (IC50)

HDAC3

11223 nM (IC50)

In Vitro

In vehicle-treated cells, α-tubulin is mainly presented in the deacetylated form, while histone 3 is clearly acetylated. Upon treatment with ACY-775, a clear enhancement of the acetylation of α-tubulin is visible, while histone acetylation remains unaltered. Acetylation of α-tubulin is visualized by immunofluorescence and the intensity in the neurites of the neurons is quantified and normalized to the length of the fluorescent signal. In vehicle-treated DRG neurons, acetylated α-tubulin is already present. Upon treatment with ACY-775 the signal intensity of acetylated α-tubulin increases significantly. Significant increase in motility of mitochondria and also the total number of mitochondria within the neurites are observed compare with vehicle-treated DRG neurons. A significantly higher number of retrogradely transport mitochondria is observed in DRG neurons treated with ACY-775 compare with vehicle-treated cells[1].

In Vivo

Biodistribution profiles of ACY-738, ACY-775, and tubastatin A are examined after acute dosing at 5 or 50 mg/kg over 2 h. At t=30 min after acute 50 mg/kg injection, respective plasma levels of ACY-738 and ACY-775 are 515 ng/mL (1.9 μM) and 1359 ng/mL (4.1 μM). Elimination from plasma is rapid, with plasmatic half-life of 12 min and concentration below 10 ng/mL after 2 h. Nevertheless, areas under concentration time curves for brain and plasm calculated over 2 h for both ACY-738 and ACY-775 lead to ratios >1. When ACY-738 (5 mg/kg) or ACY-775 (50 mg/kg) are administered repeatedly in wild-type mice at 24 h, 4 h, and 30 min before killing, significant increases in α-tubulin acetylation are observed in all tested brain regions[2].

Molecular Weight

330.36

Formula

C₁₇H₁₉FN₄O₂

CAS No.

1375466-18-4

SMILES

O=C(NO)C(C=N1)=CN=C1NC2(CCCCC2)C3=CC=CC(F)=C3

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (302.70 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0270 mL 15.1350 mL 30.2700 mL
5 mM 0.6054 mL 3.0270 mL 6.0540 mL
10 mM 0.3027 mL 1.5135 mL 3.0270 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

Undifferentiated RN46A-B14 cells, a line of immortalized rat raphe neuronal precursors, are grown. They are treated with 2.5 μM ACY-738, ACY-775, tubastatin A, 0.6 μM TSA or vehicle (0.1% DMSO) for 4 h. Samples are processed using histone extraction kit and quantified using protein assay.

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

Animal Administration
[2]

Mice are tested for immobility in the TST. At 30 min or 2 h after i.p. injection of ACY-738 (5, 50 mg/kg), ACY-775 (5, 50 mg/kg), and citalopram (0.5, 2, 20 mg/kg), a combination of the previous, or vehicle, mice are attached to the test rig and time immobile over 6 min is recorded. For open-field activity mice are injected with ACY-738 or ACY-775 at 5, 10, or 50 mg/kg or vehicle and allowed to explore. Activity is recorded[2].

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

References

Purity: 99.54%

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ACY-775
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