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Droxinostat HDAC inhibitor

Cat.No.S1422

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 HDAC inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 243.69

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 243.69 Formula

C11H14ClNO3

 Storage (From the date of receipt)
CAS No. 99873-43-5 Download SDF Storage of Stock Solutions

Synonyms NS 41080 Smiles CC1=C(C=CC(=C1)Cl)OCCCC(=O)NO

Solubility

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

Molarity Calculator

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In vivo
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Mechanism of Action

Features
Selective inhibitor of HDAC3, HDAC6,and HDAC8.
Targets/IC50/Ki
HDAC8 [3]
1.46 μM
HDAC6 [3]
2.47 μM
HDAC3 [3]
16.9 μM
HDAC9 [3]
>20 μM
HDAC10 [3]
>20 μM
HDAC1 [3]
>20 μM
HDAC2 [3]
>20 μM
HDAC4 [3]
>20 μM
HDAC5 [3]
>20 μM
HDAC7 [3]
>20 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, this compound (20 μM–60 μM) sensitizes cells to anoikis by initially activating caspase 8 with subsequent activation of the mitochondrial pathway. Similarly, it 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 this chemical remains enigma until recently. It is revealed that in histone deacetylases (HDAC) isoform 1-10, this agent 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, this compound (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
In vivo
In SCID mice models, this compound (30 μM)-treated PPC-1 cells results in decreased distant tumor formation than untreated cells. [2]
References

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