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Chemical Structure| 950762-95-5 Chemical Structure| 950762-95-5

Structure of PCI-34051
CAS No.: 950762-95-5

Chemical Structure| 950762-95-5

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PCI-34051 is a potent and selective HDAC8 inhibitor with an IC50 of 10 nM, showing more than 200-fold selectivity over other HDAC isoforms.

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Product Details of PCI-34051

CAS No. :950762-95-5
Formula : C17H16N2O3
M.W : 296.32
SMILES Code : O=C(C1=CC2=C(C=C1)C=CN2CC3=CC=C(OC)C=C3)NO
MDL No. :MFCD11114393
InChI Key :AJRGHIGYPXNABY-UHFFFAOYSA-N
Pubchem ID :24753719

Safety of PCI-34051

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

Related Pathways of PCI-34051

epigenetics

Isoform Comparison

Biological Activity

Target
  • HDAC8

    HDAC8, IC50:10 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
MV4-11 cells 50 μM PCI-34051 and KPT-9274 synergistically reduced cell survival PMC8054771
Kasumi-1 cells 50 μM PCI-34051 and KPT-9274 synergistically reduced cell survival PMC8054771
MOLM13 cells 50 μM PCI-34051 and KPT-9274 synergistically reduced cell survival PMC8054771
SK-N-BE(2)-C 6 µM 96 hours Combination treatment significantly reduced cell viability and increased the proportion of dead cells PMC6261943
Kelly 6 µM 96 hours Combination treatment significantly increased the proportion of dead cells and enhanced caspase-3 activity PMC6261943
NB-1 4 µM 96 hours Combination treatment significantly reduced cell viability and enhanced caspase-3 activity PMC6261943
HeLa cells 10 μM/20 μM 24 hours To study the role of HDAC8 as a tubulin deacetylase PMC5930436
HEK 293T cells 10 μM/20 μM 24 hours To study the role of HDAC8 as a tubulin deacetylase PMC5930436
human iPSC-derived NPCs 10 μM 24 hours PCI-34051 does not increase GRN mRNA and PGRN protein expression PMC5695697
human iPSC-derived neurons 10 μM 24 hours PCI-34051 does not increase GRN mRNA and PGRN protein expression PMC5695697
porcine oocytes 25 μmol/L and 50 μmol/L 44 hours Inhibition of HDAC8 activity led to failure of oocyte meiotic progression, showing reduced polar body extrusion rate PMC8488561
Human and murine glioma cells 1, 5, or 10 μM 24, 48, and 72 hours To evaluate the effect of PCI-34051 on cell viability, results showed that PCI-34051 reduced the viability of human and murine glioma cells. PMC8457175
CT2A glioma cells 10 μM 48 hours To evaluate the effect of PCI-34051 on cell migration, results showed that PCI-34051 inhibited the migration of CT2A glioma cells. PMC8457175

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Zebrafish Zebrafish xenograft model Surrounding water environment 15 mg/kg 30 min before CLP and 2 h and 4 h after CLP Combination treatment significantly reduced tumor volume, indicating inhibition of neuroblastoma cells PMC6261943
C57BL/6 mice Glioma model Intraperitoneal injection 100 µM 20a and 8 µM crizotinib Once daily for 48 hours To evaluate the effect of PCI-34051 on glioma growth, results showed that PCI-34051 significantly reduced tumor volume and prolonged the survival time of mice. PMC8457175

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.37mL

0.67mL

0.34mL

16.87mL

3.37mL

1.69mL

33.75mL

6.75mL

3.37mL

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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