PCI-34051

SKU: orb1300868

Description

PCI-34051

Research Area

Epigenetics & Chromatin, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 950762-95-5
• MW: 296.3
• Purity: >98%
• Formula: C₁₇H₁₆N₂O₃
• SMILES: COc1ccc(Cn2ccc3ccc(cc23)C(=O)NO)cc1
• Target: Protein deacetylase
• Solubility: Soluble in DMSO (50 mg/ml)

Bioactivity

• Target IC50:
  HDAC1:4 μM|HDAC8:10 nM|HDAC6:2.9 μM|HDAC10:13 μM
• In Vivo:
  Administration of PCI-34051 and Dexamethasone reduces eosinophilic inflammation and airway hyperresponsiveness in asthma, thereby mitigating airway remodeling .
• In Vitro:
  PCI-34051 has a good potency for HDAC8 (Ki: 10 nM). PCI-34051 has high specificity (about 5-fold) for HDAC8 relative to the other class I HDACs including HDAC1. PCI-34051 has higher 200-fold selectivity than HDAC1/6 and higher 1000-fold selectivity than HDAC2/3//10. PCI-34051 inhibits ovarian tumor line OVCAR-3 (GI50: 6 μM) and 15% cell death. Neither significant tubulin nor histone acetylation is observed in the sensitive cell lines treated with PCI-34051 (<25 μM) at 24 hours nor at earlier time points. PCI-34051 induces caspase-dependent apoptosis. When caspase-3 activity is measured at various times after treatment with 5 μM PCI-34051, increasing levels of activity are observed from 12 to 24 to 48 hours. PCI-34051 does not stimulate Bid cleavage. While J.RT3-T.5 and P116 are sensitive to PCI-34051, the PLCγ1-deficient J.gamma1 line shows a marked decrease in the extent of PCI-34051-induced apoptosis. Furthermore, steady-state calcium levels strongly influence the apoptosis induced by PCI-34051. PCI-34051 induces cytochrome c release from mitochondria.
• Cell Research:
  Cell lines: A549 cell line,Ovcar-3 cell line. Concentrations: 5 μM. Incubation Time: 24 hours. Method: Tumor cell lines and human umbilical vein endothelial cells are cultured for at least two doubling times,and growth is monitored at the end of PCI-34051 exposure using an Alamar Blue fluorometric cell proliferation assay as recommended by the manufacturer.PCI-34051 is assayed in triplicate wells in 96-well plates.The concentration required to inhibit cell growth by 50% (GI50) and 95% confidence intervals are estimated from the nonlinear regression using a four-parameter logistic equation.

Storage & Handling

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

Alternative Names

Apoptosis, inhibit, PCI 34051, PCI34051, PCI-34051, HDAC6, HDAC8, HDAC2, HDAC, HDAC10, HDAC1, Inhibitor, Histone deacetylases

Compound Identifiers

PubChem CID

24753719