PCI-34051

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.

Size Price Stock Quantity  
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.
Targets
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 M{P2VmZ2dmO2aX;uJIF{e2G7 NYfSd4E4OyCmYYnz Ml;YRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXKGenbn;0fZBmKDGkIHnu[oVkfGWmIHnuJIh2dWGwIFj1bFch[2WubIOgZYZ1\XJiMzDkZZl{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2xMlgh|ryP M4SyW|I2PDlyN{Cw
human Jurkat cells MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn\KO|IhcA>? MXvHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDKeZJs[XRiY3XscJMhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgUXRUKGG|c3H5MEBIUTVyPUGxJO69VQ>? M3LofFI{OTF4MUS3
human NB-1 cells Mn76S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV;HWm97PzJiaB?= NWOwPGhNT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVkJvMTDj[YxteyCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFNiYYPzZZktKEeLNUC9NVQh|ryP MWiyN|EyPjF2Nx?=
human MT2 cells NXS1W4pVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXi3NkBp M3vxXmdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1VOiClZXzsd{BqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTB;MUWg{txO NUfLSoJTOjNzMU[xOFc>
human MT4 cells MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXy3NkBp M1:0[mdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1VPCClZXzsd{BqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTB;MkWg{txO MV2yN|EyPjF2Nx?=

... Click to View More Cell Line Experimental Data

Protocol

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 Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
30 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
Formula

C17H16N2O3

CAS No. 950762-95-5
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID