ACY-738

SKU: orb1226416

Description

ACY-738 (ACY738) is a potent and specific HDAC6 inhibitor (IC50=1.7 nM) with improved brain bioavailability; displays 60-1500 fold selectivity over class I HDACs; induces dramatic increase in α-tubulin acetylation in brain and stimulates mouse exploratory behaviors; increases the innervation of the neuromuscular junctions in the gastrocnemius muscle and improves the motor and sensory nerve conduction in the mutant HSPB1-induced CMT2 mouse model.Depression Preclinical.

Key Properties

• CAS Number: 1375465-91-0
• MW: 270.2866
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₄N₄O₂
• SMILES: O=C(C1=CN=C(NC2(C3=CC=CC=C3)CC2)N=C1)NO
• Target: HDAC
• Solubility: DMSO: ≥ 32 mg/mL

Bioactivity

• In Vivo:
  ACY-738 (5 mg/kg) leads to significant increase in α-tubulin acetylation in whole-brain lysates. ACY-738 (50 mg/kg) fails to produce an enhancement of locomotor activity in WT mice tested in a home cage environment. ACY-738 (5 mg/kg) reaches a maximum plasma concentration of 1310 ng/mL at 0.0830 h following treatment. ACY-738 (5 mg/kg BW) alters BM B cell differentiation, but shows no significant effect on IgG and C3 deposition in NZB/W mice. ACY-738 (20 mg/kg) significantly attenuates the severity of proteinuria in NZB/W F1 mice. ACY-738 (5 mg/kg) shows a significant decrease in anti-dsDNA production in NZB/W mice as they aged. ACY-738 (5, 20 mg/kg) attenuates sera IL-1β production as the NZB/W mice aged. ACY-738 (5 mg/kg) significantly reduces glomerular IL-6 and IL-10 mRNA levels by more than 50% while treatment with 20 mg/kg ACY-738 reduced IL-6 and IL-10 mRNA to non-detectable levels.
• In Vitro:
  ACY-738 (2.5 μM) increases the acetylated (lysine 40) fraction of α-tubulin in RN46A-B14 cells. ACY-738 (10 μM) induces cell death comparable to LBH589 and FK228.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ACY738 | ACY 738

Quick Database Links

Gene Symbol

HDAC