Catalog No.S2012

PCI-34051 Chemical Structure

Molecular Weight(MW): 296.32

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.

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In DMSO USD 220 In stock
USD 170 In stock
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1 Customer Review

  • (d) Effects of HDAC8 activity on ISO-induced augmentation of apoptosis and TIPRL expression. H1299 cells were sequentially treated with 10 μm PCI-34051 for 24 h, ISO for 30 min and 50 μM cisplatin for 48 h before the western blot analysis.

    Exp Mol Med, 2017, 49(2):e297. PCI-34051 purchased from Selleck.

Purity & Quality Control

Choose Selective HDAC Inhibitors

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.
HDAC8 [1]
(Cell-free assay)
HDAC6 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
HDAC10 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
10 nM 2.9 μM 4 μM 13 μM >50 μM
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 M4LTeWZ2dmO2aX;uJIF{e2G7 MojjN{Bl[Xm| M3rTZmFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhEXiCpZX7veJlx\SBzYjDpcoZm[3SnZDDpckBpfW2jbjDIeYg4KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUC9NU45KM7:TR?= NYThW5RGOjV2OUC3NFA>
human Jurkat cells M{SxdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1:3NVczKGh? M4rZTmdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGp2emujdDDj[YxteyCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFNiYYPzZZktKEeLNUC9NVEh|ryP MXqyN|EyPjF2Nx?=
human NB-1 cells NXjQNpR3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3W3Z|czKGh? MkHiS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUmIuOSClZXzsd{BqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTB;MUSg{txO NFXadYQzOzFzNkG0Oy=>
human MT2 cells M13LdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmXoO|IhcA>? MlzkS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUXQzKGOnbHzzJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OD1zNTFOwG0> Mmm4NlMyOTZzNEe=
human MT4 cells NXTocmdJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIfjWVg4OiCq MkPoS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUXQ1KGOnbHzzJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OD1{NTFOwG0> NXvvNmFGOjNzMU[xOFc>

... Click to View More Cell Line Experimental Data


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]
+ Expand
  • 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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID