Droxinostat

SKU: orb1300731

Description

Droxinostat

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 99873-43-5
• MW: 243.69
• Purity: 99.83%
• Formula: C₁₁H₁₄ClNO₃
• SMILES: Cc1cc(Cl)ccc1OCCCC(=O)NO
• Target: Apoptosis,HDAC
• Solubility: DMSO:46 mg/mL (188.76 mM);Ethanol:46 mg/mL (188.76 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (8.21 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  HDAC6:2.47 μM|HDAC8:1.46 μM|HDAC3:16.9 μM
• In Vivo:
  In SCID mice models, Droxinostat (30 μM)-treated PPC-1 cells results in decreased distant tumor formation than untreated cells.
• In Vitro:
  Droxinostat is originally identified as a sensitizer of PPC-1 cells to FAS and TRAIL by downregulatin the expression of c-Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein (c-FLIP). In PPC-1 cells cultured in suspension but not adherent conditions, Droxinostat (20 μM–60 μM) sensitizes cells to anoikis by initially activating caspase 8 with subsequent activation o the mitochondrial pathway. Similarly, Droxinostat also sensitizes Other cancer cell lines including PC-3, DU-145, T47D, and OVCAR-3, but not LNCaP or MB-MDA-468, to anoikis or CH-11-induced apoptosis. however the Direct targets of Droxinostat remains enigma until recently. It is revealed that in histone deacetylases (HDAC) isoform 1-10, Droxinostat Selective inhibits HDAC3, 6, and 8, with IC50 Values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively without inhibiting Other HDAC members IC50 > 20 μM). In MCF-7 breast cancer cells, Droxinostat (10 μM–100 μM) sensitizes cells to apoptosis by decreasing c-FLIPL and c-FLIPS expression, reducing cell survival, and inducing apoptosis.
• Cell Research:
  PPC-1 cells (1 × 10^4 are seeded overnight into 96-well flat-bottomed plates in 100 μL of medium containing 2.5% FCS the Next day, Droxinostat is added. CH-11 antibody (100 ng/mL) is then added an the cells are incubated for 24 hours before assessing cell viability by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) dye reduction assay.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Droxinostat, cancer, Apoptosis, NS41080, NS-41080, NS 41080, inhibit, Inhibitor, hepatocellular carcinoma (HCC), HDAC9, HDAC8, HDAC3, HDAC6, HDAC, HDAC10, histone deacetylase (HDAC), Histone deacetylases

Compound Identifiers

PubChem CID

568416