1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. Droxinostat

Droxinostat (Synonyms: NS 41080)

Cat. No.: HY-13267 Purity: 98.86%
Handling Instructions

Droxinostat(NS41080) is a selective inhibitor of HDAC3, HDAC6, and HDAC8 with IC50 of 16.9, 2.47 and 1.46 μM, respectively; > 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.

For research use only. We do not sell to patients.

Droxinostat Chemical Structure

Droxinostat Chemical Structure

CAS No. : 99873-43-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 72 In-stock
Estimated Time of Arrival: December 31
5 mg USD 65 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 456 In-stock
Estimated Time of Arrival: December 31
100 mg USD 734 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Droxinostat(NS41080) is a selective inhibitor of HDAC3, HDAC6, and HDAC8 with IC50 of 16.9, 2.47 and 1.46 μM, respectively; > 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10. IC50 Value: 16.9 μM(HDAC3); 2.47 μM(HDAC6); 1.46 μM(HDAC8) Target: HDAC3/6/8 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). 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). 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. in vivo: In SCID mice models, Droxinostat (30 μM)-treated PPC-1 cells results in decreased distant tumor formation than untreated cells.

IC50 & Target[2]

HDAC8

1.46 μM (IC50)

HDAC6

2.47 μM (IC50)

HDAC3

16.9 μM (IC50)

Molecular Weight

243.69

Formula

C₁₁H₁₄ClNO₃

CAS No.

99873-43-5

SMILES

ClC1=CC=C(C(C)=C1)OCCCC(NO)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (615.54 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1036 mL 20.5179 mL 41.0357 mL
5 mM 0.8207 mL 4.1036 mL 8.2071 mL
10 mM 0.4104 mL 2.0518 mL 4.1036 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 98.86%

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Droxinostat
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