PCI-34051

SKU: orb1223540

Description

PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM. It has greater than 200-fold selectivity over HDAC1 and 6, more than 1000-fold selectivity over HDAC2, 3, and 10.

Key Properties

• CAS Number: 950762-95-5
• MW: 296.32
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₆N₂O₃
• SMILES: O=C(C1=CC2=C(C=C1)C=CN2CC3=CC=C(OC)C=C3)NO
• Target: HDAC
• Solubility: DMSO:59 mg/mL (199.1 mM); Ethanol:<1 mg/mL (<1 mM); Water:<1 mg/mL (<1 mM)

Bioactivity

• In Vivo:
  Administration of PCI-34051 and Dexamethasone reduces the eosinophilic inflammation and airway hyperresponsiveness in asthma to reduce the airway remodeling.
• In Vitro:
  PCI-34051 inhibits pure recombinant HDAC8 with Ki of 10 nM with >200-fold selectivity over the other HDACs tested, including HDACs 1, 2, 3, 6 and 10. PCI-34051 is derived from a low molecular weight hydroxamic acid scaffold that possessed promising potency (HDAC8; Ki=2 μM) and selectivity (approximately fivefold) for HDAC8 relative to the other class I HDACs. PCI-34051 is found to induce apoptosis at low micromolar concentrations in cell lines derived from T-cell lymphomas, including Jurkat and HuT78, whereas doses as high as 20 μM has no effect on B-cell- or myeloid-derived lymphomas or solid tumor lines.

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

PCI34051 | PCI 34051 | PCI-34051

Quick Database Links

Gene Symbol

HDAC