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ACY-775

Catalog No. TQ0074 CAS 1375466-18-4

ACY-775 is an effective and specific inhibitor of HDAC6 (IC50: 7.5 nM).

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ACY-775, CAS 1375466-18-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
2 mg	In stock	$ 43.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 255.00
50 mg	In stock	$ 413.00
100 mg	In stock	$ 618.00
500 mg	In stock	$ 1,330.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 97.67%

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Description	ACY-775 is an effective and specific inhibitor of HDAC6 (IC50: 7.5 nM).
Targets&IC50	HDAC6:7.5 nM, HDAC1:2123 nM
In vitro	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. A significant increase in motility of mitochondria and also the total number of mitochondria within the neurites are observed compared with vehicle-treated DRG neurons. A significantly higher number of retrogradely transport mitochondria is observed in DRG neurons treated with ACY-775 compared with vehicle-treated cells [1].
In vivo	Biodistribution profiles of ACY-775 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-775 is 1359?ng/mL (4.1?μM). Elimination from the plasma is rapid, with a plasmatic half-life of 12?min and a concentration below 10?ng/mL after 2?h. When ACY-775 (50?mg/kg) is 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].
Cell Research	Undifferentiated RN46A-B14 cells 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 a histone extraction kit and quantified using protein assay [2].
Animal Research	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 [2].

Molecular Weight	330.36
Formula	C17H19FN4O2
CAS No.	1375466-18-4

Storage

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

Solubility Information

DMSO: 100 mg/mL (302.70 mM), Sonification and heating are recommended.

References and Literature

1. Veronick Benoy, et al. Development of Improved HDAC6 Inhibitors as Pharmacological Therapy for Axonal Charcot-Marie-Tooth Disease. Neurotherapeutics. 2017 Apr; 14(2): 417-428. 2. Jeanine Jochems et al. Antidepressant-Like Properties of Novel HDAC6-Selective Inhibitors with Improved Brain Bioavailability. Neuropsychopharmacology. 2014 Jan; 39(2): 389-400.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Epigenetics Compound Library Chromatin Modification Compound Library Reprogramming Compound Library NF-κB Signaling Compound Library NO PAINS Compound Library Anti-Breast Cancer Compound Library Bioactive Compound Library Anti-Pancreatic Cancer Compound Library DNA Damage & Repair Compound Library

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Keywords

ACY-775 1375466-18-4 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Histone deacetylases inhibit ACY 775 Inhibitor ACY775 inhibitor

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