DroxinostatA selective inhibitor of HDAC3, HDAC6, and HDAC8

Droxinostat (CAS 99873-43-5)

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Synonym: 4-(4-Chloro-2-methylphenoxy)-N-hydroxybutanamide
Application: A selective inhibitor of HDAC3, HDAC6, and HDAC8
CAS Number: 99873-43-5
Molecular Weight: 243.69
Molecular Formula: C11H14ClNO3
* Refer to Certificate of Analysis for lot specific data (including water content).
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Droxinostat selectively inhibits HDAC3, 6, and 8, with IC50 values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively Droxinostat is originally identified as a sensitizer of PPC-1 cells to FAS and TRAIL by down-regulating the expression of c-Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein (c-FLIP). In PPC-1 cells were cultured in suspension but not adherent conditions. 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. 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.

Physical State :
Solid
Solubility :
Soluble in DMSO (49 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (49 mg/ml at 25 °C).
Storage :
Store at -20° C
Melting Point :
170.63 °C (Predicted)
Boiling Point :
423.48 °C (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.55 (Predicted)
IC50 :
HDAC8: IC50 = 1.46 µM; HDAC6: IC50 = 2.47 µM; HDAC3: IC50 = 16.9 µM; Mycobacterium Tuberculosis: IC50 = 17.59 µM; Mycobacterium tuberculosis H37Rv: IC50 >28.64 µM
pK Values :
pKa: 9.32 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
568416
MDL Number :
MFCD01326592
SMILES :
CC1=C(C=CC(=C1)Cl)OCCCC(=O)NO

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Certificate of Analysis

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Droxinostat  Product Citations

See how others have used Droxinostat. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 26519528  Stammler, D. et al. 2015. J. Immunol. 195: 5421-31.

Citations 1 to 1 of 1 total
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