Home Cytoskeletal Signaling HDAC inhibitor Droxinostat For research use only.

Droxinostat

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.

Droxinostat Chemical Structure

Droxinostat Chemical Structure

CAS: 99873-43-5

Selleck's Droxinostat has been cited by 13 Publications

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Purity & Quality Control

Batch: S142201 DMSO] 49 mg/mL] false] Ethanol] 49 mg/mL] false] Water] Insoluble] false Purity: 99.88%
99.88

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Biological Activity

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.
Features Selective inhibitor of HDAC3, HDAC6,and HDAC8.
Targets
HDAC8 [3] HDAC6 [3] HDAC3 [3] HDAC9 [3] HDAC10 [3] Click to View More Targets
1.46 μM 2.47 μM 16.9 μM >20 μM >20 μM
In vitro
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]
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 Cell lines PPC-1 cells
Concentrations 0–100 μM, dissolved in DMSO (final concentration of DMSO is 0.5%)
Incubation Time 24 hours
Method 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.
In Vivo
In vivo In SCID mice models, Droxinostat (30 μM)-treated PPC-1 cells results in decreased distant tumor formation than untreated cells. [2]

Chemical lnformation & Solubility

Molecular Weight 243.69 Formula

C11H14ClNO3
CAS No. 99873-43-5 SDF Download Droxinostat SDF
Smiles CC1=C(C=CC(=C1)Cl)OCCCC(=O)NO
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 49 mg/mL ( (201.07 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 49 mg/mL

Water : Insoluble


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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