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Catalog No.S2012

37 publications

PCI-34051 Chemical Structure

CAS No. 950762-95-5

PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM in a cell-free assay. It has greater than 200-fold selectivity over HDAC1 and 6, more than 1000-fold selectivity over HDAC2, 3, and 10. PCI-34051 induces caspase-dependent apoptosis.

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10mM (1mL in DMSO) USD 220 In stock
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Selleck's PCI-34051 has been cited by 37 publications

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Biological Activity

Description PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM in a cell-free assay. It has greater than 200-fold selectivity over HDAC1 and 6, more than 1000-fold selectivity over HDAC2, 3, and 10. PCI-34051 induces caspase-dependent apoptosis.
HDAC8 [1]
(Cell-free assay)
10 nM
In vitro

PCI-34051 possesses promising potency for HDAC8 with a Ki of 10 nM. PCI-34051 has high selectivity (approximately fivefold) for HDAC8 relative to the other class I HDACs including HDAC1. PCI-34051 reveals greater than 200-fold selectivity over HDAC1 and HDAC6, and greater than 1000-fold selectivity over HDAC2, HDAC3 and HDAC10. PCI-34051 inhibits ovarian tumor line OVCAR-3 with a GI50 of 6 μM and 15% cell death. Neither significant tubulin nor histone acetylation is observed in the sensitive cell lines treated with PCI-34051 at concentrations less than 25 μM at 24 hours nor at earlier timepoints. PCI-34051 induces a selective cytotoxic effect in cell lines derived only from T-cell malignancies. PCI-34051 induces caspase-dependent apoptosis. When caspase-3 activity is measured at various times after treatment with 5 μM PCI-34051, increasing levels of activity are observed from 12 to 24 to 48 hours, another hallmark of apoptosis, consistent with the higher levels of caspase activity at this timepoint. PCI-34051 does not stimulate Bid cleavage, a characteristic effect of the extrinsic apoptotic pathway. While P116 and J.RT3-T.5 are sensitive to PCI-34051, the PLCγ1-deficient J.gamma1 line reveals a marked decrease in the extent of PCI-34051-induced apoptosis. In addition, steady-state calcium levels strongly influence the apoptosis induced by PCI-34051. PCI-34051 induces cytochrome c release from mitochondria.[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human Huh7 cells MVXGeY5kfGmxbjDhd5NigQ>? MU[zJIRigXN? MmjGRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXKGenbn;0fZBmKDGkIHnu[oVkfGWmIHnuJIh2dWGwIFj1bFch[2WubIOgZYZ1\XJiMzDkZZl{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2xMlgh|ryP MWmyOVQ6ODdyMB?=
human Jurkat cells NVT3b4l7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWq3NkBp M{X6[Gdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGp2emujdDDj[YxteyCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFNiYYPzZZktKEeLNUC9NVEh|ryP M4roSFI{OTF4MUS3
human NB-1 cells M2ntXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHX0SpI4OiCq MXfHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDORk0yKGOnbHzzJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OD1zNDFOwG0> MoPnNlMyOTZzNEe=
human MT2 cells NYj3UFBCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVu3NkBp MYXHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNWFIh[2WubIOgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxRTF3IN88US=> NGXJcWEzOzFzNkG0Oy=>
human MT4 cells MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUXR[JNLPzJiaB?= NFX3d4RIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOXDRiY3XscJMhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgUXRUKGG|c3H5MEBIUTVyPUK1JO69VQ>? MlXUNlMyOTZzNEe=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
SMC3 / Ac-SMC3 ; 

PubMed: 27072133     

A and B, representative immunofluorescence analysis of total- and ac-SMC3 in G1-S synchronized MCF7 cells treated with the indicated concentrations of PCI-34051 for 6 and 12 h, respectively. MCF7 cells grown in complete medium were synchronized to G1-S phase by double thymidine block and released in the presence of different concentrations of PCI-34051 for 6 or 12 h. Cells were stained for DNA (Hoechst-H33342, blue) and with antibodies detecting total-SMC3 (green) and ac-SMC3 (red). Cells were analyzed by Nikon C2 confocal microscope; images were taken at 20× magnification (z-series) using the NIS elements software, z-stacked, and processed using FIJI.



Kinase Assay:[1]
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Histone deacetylase activity:

For PCI-34051 characterization, measurements are perfomed in a reaction volume of 100 μL using 96-well assay plates in a fluorescence plate reader. For each isozyme. The HDAC protein in reaction buffer (50 mM HEPES, 100 mM KCl, 0.001% Tween-20, 5% dimethyl sulfoxide, pH7.4, supplemented with bovine serum albumin at concentrations of 0-0.05%) is mixed with PCI-34051 at various concentrations and allowed to incubate for 15 min. Trysin is added to a final concentration of 50 nM, and acetyl-gly-Ala-(N-acetyl-Lys)-amino-4-methylcoumarin is added to a final concentration of 25-100 μM to initiate the reaction. After a 30 min lag time, the fluorescence is measured over a 30 min time frame using an excitation wavelength of 335 nm and a detection wavelength of 460 nm. The increase in fluorescence wih time is used as the measure of the reaction rate.
Cell Research:[1]
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  • Cell lines: A549 cell line, Ovcar-3 cell line
  • Concentrations: 5 μM
  • Incubation Time: 24 hours
  • Method: Tumor cell lines and human umbilical vein endothelial cells are cultured for at least two doubling times, and growth is monitored at the end of PCI-34051 exposure using an Alamar Blue fluorometric cell proliferation assay as recommended by the manufacturer. PCI-34051 is assayed in triplicate wells in 96-well plates. The concentration required to inhibit cell growth by 50% (GI50) and 95% confidence intervals are estimated from nonlinear regression using a four-parameter logistic equation.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 59 mg/mL (199.1 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40%PEG300+5% tween80+50% H2O
For best results, use promptly after mixing.
5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 296.32


CAS No. 950762-95-5
Storage powder
in solvent
Synonyms N/A
Smiles COC1=CC=C(C=C1)CN2C=CC3=C2C=C(C=C3)C(=O)NO

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID