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Droxinostat

Catalog No. T6481 CAS 99873-43-5

Synonyms: NS 41080

Droxinostat (NS 41080) is a selective inhibitor of HDAC, mostly for HDACs 6 and 8 with IC50 of 2.47 μM and 1.46 μM, greater than 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Droxinostat, CAS 99873-43-5

Pack Size	Availability	Price/USD
2 mg	In stock	$ 31.00
5 mg	In stock	$ 46.00
10 mg	In stock	$ 87.00
25 mg	In stock	$ 185.00
50 mg	In stock	$ 278.00
100 mg	In stock	$ 413.00
1 mL * 10 mM (in DMSO)	In stock	$ 47.00

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Purity: 99.76%

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Description	Droxinostat (NS 41080) is a selective inhibitor of HDAC, mostly for HDACs 6 and 8 with IC50 of 2.47 μM and 1.46 μM, greater than 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.
Targets&IC50	HDAC6:2.47 μM, HDAC8:1.46 μM
In vitro	Droxinostat is originally identified as a sensitizer of PPC-1 cells to FAS and TRAIL by downregulating the expression of c-Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein (c-FLIP). [1] 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 of 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. [2] 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). [3] 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. [4]
In vivo	In SCID mice models, Droxinostat (30 μM)-treated PPC-1 cells results in decreased distant tumor formation than untreated cells. [2]
Kinase Assay	HDAC Inhibition Assay: HDAC inhibition is assessed using the CycLex HDACs fluorometric assay according to the manufacturer's protocol and using crude nuclear extract from HeLa cells (principally HDAC1 and HDAC2). The relative activity is expressed as (fluorescence intensity of treated samples/fluorescence intensity of controls) × 100
Cell Research	PPC-1 cells (1 × 104) 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 and 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)

Synonyms	NS 41080
Molecular Weight	243.69
Formula	C11H14ClNO3
CAS No.	99873-43-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 46 mg/mL (188.8 mM)

Ethanol: 46 mg/mL (188.8 mM)

References and Literature

1. Schimmer AD, et al. Cancer Res, 2006, 66(4), 2367-2375. 2. Mawji IA, et al. J Natl Cancer Inst, 2007, 99(10), 811-822. 3. Wood TE, et al. Mol Cancer Ther, 2010, 9(1), 246-256. 4. Bijangi-Vishehsaraei K, et al. Mol Cell Biochem, 2010, 342(1-2), 133-142.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Pancreatic Cancer Compound Library Histone Modification Compound Library Reprogramming Compound Library Anti-Cancer Compound Library Immunology/Inflammation Compound Library DNA Damage & Repair Compound Library Autophagy Compound Library Bioactive Compounds Library Max NO PAINS Compound Library

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Keywords

Droxinostat 99873-43-5 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair HDAC HDAC3 hepatocellular carcinoma (HCC) NS41080 Histone deacetylases cancer inhibit NS-41080 NS 41080 HDAC6 HDAC8 Inhibitor histone deacetylase (HDAC) inhibitor

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