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Droxinostat

Cat. No. M1993

All AbMole products are for research use only, cannot be used for human consumption.

Droxinostat Structure
Synonym:

NS 41080

Size Price Availability Quantity
5mg USD 56  USD56 In stock
10mg USD 95  USD95 In stock
50mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

Droxinostat is originally identified as a sensitizer of PPC-1 cells to FAS and TRAIL by down-regulating the expression of c-Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein (c-FLIP). Droxinostat also downregulated c-FLIP expression, induced caspase-8- and caspase-3/7-mediated apoptosis, and increased apoptosis in bicalutamide-treated cells. Droxinostat shows a significant action on gene transcription hence controlling tumor progression. Droxinostat (10 μM - 100 μM) sensitizes cells to apoptosis by decreasing c-FLIPL and c-FLIPS expression, reducing cell survival, and inducing apoptosis in MCF-7 breast cancer cells. In SCID mice models, Droxinostat (30 μM)-treated PPC-1 cells results in decreased distant tumor formation than untreated cells.

Protocol (for reference only)
Cell Experiment
Cell lines PPC-1 cells
Preparation method Viability of PPC-1 cells treated with 5809354 or 7271570 (0, 20, 40, 60, and 80 μM) with and without CH-11 (100 ng/mL) or cultured under adherent or suspension conditions and MEFs treated with 5809354 (0, 20, 40, 60, and 80 μM) under adherent or suspension conditions was assessed using the 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium inner salt reduction assay (Promega, Madison, WI) according to the manufacturer's protocols as previous described (18). The percent relative cell viability was expressed as (optical density of treated cells/optical density of controls) × 100%. Two independent experiments were performed in triplicate (n = 6).
Concentrations 0, 20, 40, 60, and 80 μM
Incubation time 30 h
Animal Experiment
Animal models male SCID mice between 5 and 7 weeks of age prostate cancer cells in vivo
Formulation PBS
Dosages 30 μM
Administration i.p.
Chemical Information
Molecular Weight 243.69
Formula C11H14ClNO3
CAS Number 99873-43-5
Solubility (25°C) DMSO 40 mg/mL
Ethanol 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] McCourt C, et al. Clin Cancer Res. Elevation of c-FLIP in castrate-resistant prostate cancer antagonizes therapeutic response to androgen receptor-targeted therapy.

[2] Bijangi-Vishehsaraei K, et al. Mol Cell Biochem. 4-(4-Chloro-2-methylphenoxy)-N-hydroxybutanamide (CMH) targets mRNA of the c-FLIP variants and induces apoptosis in MCF-7 human breast cancer cells.

[3] Wood TE, et al. Mol Cancer Ther. Selective inhibition of histone deacetylases sensitizes malignant cells to death receptor ligands.

[4] Mawji IA, et al. J Natl Cancer Inst. Critical role for Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein in anoikis resistance and distant tumor formation.

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Keywords: Droxinostat, NS 41080 supplier, HDAC, inhibitors, activators

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