Quisinostat

SKU: orb1301114

Description

Quisinostat

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 875320-29-9
• MW: 394.47
• Purity: ≥98% (May vary between batches)
• Formula: C₂₁H₂₆N₆O₂
• SMILES: Cn1cc(CNCC2CCN(CC2)c2ncc(cn2)C(=O)NO)c2ccccc12
• Target: Apoptosis|||HDAC|||Autophagy
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.07 mM);DMSO:126.25 mg/mL (320.05 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  HDAC5:3.69 nM|HDAC9:32.1 nM|HDAC7:119 nM|HDAC2:0.33 nM|HDAC1:0.11 nM|HDAC4:0.64 nM|HDAC8:4.26 nM|HDAC6:76.8 nM|HDAC10:0.46 nM|HDAC3:4.86 nM|HDAC11:0.37 nM
  Read more...
• In Vivo:
  Quisinostat induces continuous H3 acetylation in tumor tissue in vivo. Quisinostat, a "second-generation" HDAC inhibitor with prolonged pharmacodynamic response in vivo. In agreement with the hypothesis, Quisinostat showed superior efficacy compared with both standard of care agents and first-generation HDAC inhibitors in preClinicalal tumor models. These studies suggest that an HDAC inhibitor with continuous pharmacodynamic activity may show activity in solid tumor malignancies.
  Read more...
• In Vitro:
  Quisinostat exerts broad-spectrum antiproliferative activity against a wide panel of cancer cell lines including lung, colon, breast, prostate, and ovarian cell lines at nanomolar concentrations. JNJ-26481585 shows activity toward all HDAC enzymes tested with highest potency in vitro observed toward recombinant HDAC1 (IC50, 0.11±0.03 nM), which is comparable with the potency observed toward HDAC1-immunoprecipitated complexes from tumor cells (IC50, 0.16±0.02 nM). Lowest in vitro potency is observed toward HDAC6, 7 and 9 (IC50, 32.1-119 nM) .
  Read more...

Storage & Handling

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

Alternative Names

deacetylase, Inhibitor, hematologic, HDAC, HDAC10, HDAC11, HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC8, malignancies, Histone deacetylases, histone, inhibit, JNJ 26481585, JNJ26481585, JNJ-26481585, Apoptosis, Autophagy, Quisinostat

Compound Identifiers

PubChem CID

11538455