ACY-738

SKU: orb1304133

Description

ACY-738 is a potent and selective HDAC6 inhibitor with an IC50 of 1.7 nM, exhibiting approximately 100-fold selectivity over Class I HDACs. This small molecule is a valuable research tool for investigating HDAC6 biology in cellular and animal models of oncology, neurology, and immunology.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1375465-91-0
• MW: 270.29
• Purity: 99.89% (May vary between batches)
• Formula: C₁₄H₁₄N₄O₂
• SMILES: N(C1(CC1)C2=CC=CC=C2)C=3N=CC(C(NO)=O)=CN3
• Target: HDAC
• Solubility: DMSO:50 mg/mL (184.99 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.4 mM)

Bioactivity

• Target IC50:
  HDAC2:128 nM|HDAC1:94 nM|HDAC6:1.7 nM|HDAC3:218 nM
• In Vivo:
  ACY-738 administered at a dosage of 5 mg/kg notably increases α-tubulin acetylation in whole-brain lysates, whereas a higher dosage (50 mg/kg) fails to enhance locomotor activity in wild-type (WT) mice within a home cage setting. At a dosage of 5 mg/kg by body weight (BW), ACY-738 influences B cell differentiation in bone marrow (BM) without significantly impacting immunoglobulin G (IgG) and complement component 3 (C3) deposition in NZB/W mice. This dosage also achieves a peak plasma concentration of 1310 ng/mL approximately 0.0830 hours post-treatment. When the dosage is increased to 20 mg/kg, ACY-738 markedly reduces the severity of proteinuria in NZB/W F1 mice and significantly lowers anti-double-stranded DNA (anti-dsDNA) production as well as glomerular interleukin-6 (IL-6) and interleukin-10 (IL-10) mRNA levels by more than 50% in NZB/W mice; the latter being reduced to non-detectable levels with the 20 mg/kg treatment. Additionally, both 5 and 20 mg/kg dosages of ACY-738 decrease serum interleukin-1 beta (IL-1β) production as the NZB/W mice age.
• In Vitro:
  ACY-738 increases the acetylated (lysine 40) fraction of α-tubulin in RN46A-B14 cells at the concentration of 2.5 μM. The effect that ACY-738 (10 μM) induces cell death is similar to LBH589 and FK228.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ACY738, ACY-738, ACY 738, inhibit, HDAC6, HDAC, Inhibitor, Histone deacetylases

Compound Identifiers

PubChem CID

57381425