DroxinostatSelective HDAC inhibitor CAS# 99873-43-5 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 99873-43-5 | SDF | Download SDF |
| PubChem ID | 568416 | Appearance | Powder |
| Formula | C11H14ClNO3 | M.Wt | 243.69 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | NS 41080 | ||
| Solubility | DMSO : ≥ 150 mg/mL (615.54 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 4-(4-chloro-2-methylphenoxy)-N-hydroxybutanamide | ||
| SMILES | CC1=C(C=CC(=C1)Cl)OCCCC(=O)NO | ||
| Standard InChIKey | JHSXDAWGLCZYSM-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C11H14ClNO3/c1-8-7-9(12)4-5-10(8)16-6-2-3-11(14)13-15/h4-5,7,15H,2-3,6H2,1H3,(H,13,14) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Droxinostat is a selective inhibitor of HDAC with IC50 values of 2.47 μM and 1.46 μM for HDACs 6 and 8, respectively. | ||||||
| Targets | HDAC8 | HDAC6 | HDAC3 | HDAC1 | HDAC2 | ||
| IC50 | 1.46 μM | 2.47 μM | 16.9 μM | >20 μM | >20 μM | ||
Droxinostat Dilution Calculator
Droxinostat Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 4.1036 mL | 20.5179 mL | 41.0357 mL | 82.0715 mL | 102.5894 mL |
| 5 mM | 0.8207 mL | 4.1036 mL | 8.2071 mL | 16.4143 mL | 20.5179 mL |
| 10 mM | 0.4104 mL | 2.0518 mL | 4.1036 mL | 8.2071 mL | 10.2589 mL |
| 50 mM | 0.0821 mL | 0.4104 mL | 0.8207 mL | 1.6414 mL | 2.0518 mL |
| 100 mM | 0.041 mL | 0.2052 mL | 0.4104 mL | 0.8207 mL | 1.0259 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Droxinostat is a selective inhibitor of HDAC3, HDAC6, and HDAC8 with IC50 value of 16.9 ± 5.0 μM, 2.47 ± 1.09 μM, and 1.46 ± 0.11 μM, respectively [1].
HDACs (histone deacetylases) are enzymes responsible of the deacetylation of lysine that residues of core histones and play a pivotal role in controlling chromatin remodeling and transcriptional activation. It is also reported that HDACs control the acetylation and activation status of multiple non-histone proteins, including the heat shock protein 90 (Hsp90) which is an essential molecular chaperone for fungal virulence and antifungal resistance. Multiple HDACs have been identified and HDAC1 to HDAC10 are shown to express in malignant cells which reminds the HDAC inhibitor as a target for cancer therapy [2] [3].
Droxinostat is a selective HDAC inhibitor and is different from the known pan-HDACi TSA which inhibits all tested HDAC. When tested with prostate cancer line PPC-1 cells, droxinostat treatment selectively inhibited HDAC3, HDAC6, and HDAC8 activity at the concentration of 50 μM/L which sensitized cells to death ligands [1]. In androgen-dependent CaP cells, administration of droxinostat selectively inhibited HDACs and downregulated c-FLP expression which resulted in cells apoptosis [4].
References:
[1]. Wood, T.E., et al., Selective inhibition of histone deacetylases sensitizes malignant cells to death receptor ligands. Mol Cancer Ther, 2010. 9(1): p. 246-56.
[2]. Lamoth, F., P.R. Juvvadi, and W.J. Steinbach, Histone deacetylase inhibition as an alternative strategy against invasive aspergillosis. Front Microbiol, 2015. 6: p. 96.
[3]. Mackmull, M.T., et al., Histone deacetylase inhibitors cause the selective depletion of bromodomain containing proteins. Mol Cell Proteomics, 2015.
[4]. McCourt, C., et al., Elevation of c-FLIP in castrate-resistant prostate cancer antagonizes therapeutic response to androgen receptor-targeted therapy. Clin Cancer Res, 2012. 18(14): p. 3822-33.
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Droxinostat, a Histone Deacetylase Inhibitor, Induces Apoptosis in Hepatocellular Carcinoma Cell Lines via Activation of the Mitochondrial Pathway and Downregulation of FLIP.[Pubmed:26947884]
Transl Oncol. 2016 Feb;9(1):70-78.
BACKGROUND: The current chemotherapeutic outcomes for hepatocellular carcinoma (HCC) are not encouraging, and long-term survival of this patient group remains poor. Recent studies have demonstrated the utility of histone deacetylase inhibitors that can disrupt cell proliferation and survival in HCC management. However, the effects of Droxinostat, a type of histone deacetylase inhibitor, on HCC remain to be established. METHODS: The effects of Droxinostat on HCC cell lines SMMC-7721 and HepG2 were investigated. Histone acetylation and apoptosis-modulating proteins were assessed via Western blot. Proliferation was examined with 3-(4, 5 dimetyl-2-thiazolyl)-2, 5-diphenyl 2H-tetrazolium bromide, cell proliferation, and real-time cell viability assays, and apoptosis with flow cytometry. RESULTS: Droxinostat inhibited proliferation and colony formation of the HCC cell lines examined. Hepatoma cell death was induced through activation of the mitochondrial apoptotic pathway and downregulation of FLIP expression. Droxinostat suppressed histone deacetylase (HDAC) 3 expression and promoted acetylation of histones H3 and H4. Knockdown of HDAC3 induced hepatoma cell apoptosis and histone H3 and H4 acetylation. CONCLUSIONS: Droxinostat suppresses HDAC3 expression and induces histone acetylation and HCC cell death through activation of the mitochondrial apoptotic pathway and downregulation of FLIP, supporting its potential application in the treatment of HCC.
