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Droxinostat HDAC inhibitor

Name: Droxinostat
Brand: Selleck Chemicals
SKU: S1422
Availability: InStock
Rating: 5 (14 reviews)

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.

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%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.88

Related Targets	Akt Wnt/beta-catenin PKC HSP ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK
Other HDAC Inhibitors	ITF-2357 (Givinostat) Hydrochloride Monohydrate Fimepinostat (CUDC-907) Trichostatin A (TSA) Entinostat (MS-275) RGFP966 Quisinostat (JNJ-26481585) Dihydrochloride Tubastatin A HCl Tubastatin A Mocetinostat (MGCD0103) Ricolinostat (ACY-1215)

Solubility

In vitro
Batch:

DMSO : 49 mg/mL (201.07 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 49 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%propylene glycol 1 5%Tween80 2 65%D5W Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (123.11mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	243.69	Formula	C₁₁H₁₄ClNO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	99873-43-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NS 41080			Smiles	CC1=C(C=CC(=C1)Cl)OCCCC(=O)NO

Mechanism of Action

Features	Selective inhibitor of HDAC3, HDAC6,and HDAC8.
Targets/IC₅₀/Ki	HDAC8 1.46 μM HDAC6 2.47 μM HDAC3 16.9 μM HDAC9 >20 μM HDAC10 >20 μM HDAC1 >20 μM HDAC2 >20 μM HDAC4 >20 μM HDAC5 >20 μM HDAC7 >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). 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. 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). In MCF-7 breast cancer cells, this compound (10 μM–100 μM) sensitizes cells to apoptosis by decreasing c-FLIP_L and c-FLIP_S expression, reducing cell survival, and inducing apoptosis.
Kinase Assay	HDAC Inhibition Assay
Kinase 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16489043/ [2] https://pubmed.ncbi.nlm.nih.gov/17505076/ [3] https://pubmed.ncbi.nlm.nih.gov/20053768/ [4] https://pubmed.ncbi.nlm.nih.gov/20446019/

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