ACY-775

SKU: orb1296224

Description

ACY-775

Research Area

Product Categories/Products/Small Molecules,Chromatin/Epigenetic|||DNA Damage/DNA Repair

Key Properties

• CAS Number: 1375466-18-4
• MW: 330.36
• Purity: 97.67%
• Formula: C₁₇H₁₉FN₄O₂
• SMILES: ONC(=O)c1cnc(NC2(CCCCC2)c2cccc(F)c2)nc1

Bioactivity

• Target IC50:
  HDAC6:7.5 nM|HDAC3:11223 nM|HDAC1:2123 nM|HDAC2:2570 nM
• 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 .
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• 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 .
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• 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 .
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• 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 .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Compound Identifiers

PubChem CID

57382288