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Chemical Structure| 99873-43-5 Chemical Structure| 99873-43-5

Structure of Droxinostat
CAS No.: 99873-43-5

Chemical Structure| 99873-43-5

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Droxinostat is an inhibitor of HDAC3, HDAC6, and HDAC8 with IC50 of 16.9, 2.47 and 1.46 μM, respectively.

Synonyms: NS 41080

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Product Details of Droxinostat

CAS No. :99873-43-5
Formula : C11H14ClNO3
M.W : 243.69
SMILES Code : ClC1=CC=C(C(C)=C1)OCCCC(NO)=O
Synonyms :
NS 41080
MDL No. :MFCD01326592
InChI Key :JHSXDAWGLCZYSM-UHFFFAOYSA-N
Pubchem ID :568416

Safety of Droxinostat

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Droxinostat

epigenetics

Isoform Comparison

Biological Activity

Target
  • HDAC8

    HDAC8, IC50:1.46 μM

  • HDAC3

    HDAC3, IC50:16.9 μM

  • HDAC6

    HDAC6, IC50:2.47 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
LNCaP cells 60 μM Repressed c-FLIP expression and induced PARP cleavage, promoting apoptosis PMC3512078
22Rv1 cells 30 μM Repressed c-FLIP expression and induced PARP cleavage, promoting apoptosis PMC3512078
HT-29 colon cancer cells 21 μM 12 or 24 hours To evaluate the effect of Droxinostat on HT-29 cell growth, results showed that Droxinostat significantly inhibited cell growth and induced cellular apoptosis and ROS production. PMC6064062
SMMC-7721 0, 10, 20, 40, 80 μM 96 hours Droxinostat inhibited proliferation and colony formation of SMMC-7721 cells, inducing apoptosis through activation of the mitochondrial apoptotic pathway and downregulation of FLIP expression. PMC4800063
HepG2 0, 10, 20, 40, 80 μM 96 hours Droxinostat inhibited proliferation and colony formation of HepG2 cells, inducing apoptosis through activation of the mitochondrial apoptotic pathway and downregulation of FLIP expression. PMC4800063
HDAC8 2 mM To study the binding mode of Droxinostat with HDAC8 PMC6903415

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Bleomycin-induced pulmonary fibrosis model Oropharyngeal aspiration 30 µM Single dose, continued until day 14 Reduced FLIP expression, increased Ku70 acetylation, decreased Ku70/FLIP complex, and attenuated pulmonary fibrosis PMC7408087

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.10mL

0.82mL

0.41mL

20.52mL

4.10mL

2.05mL

41.04mL

8.21mL

4.10mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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