PCI-34051

Catalog No.S2012

For research use only.

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.

PCI-34051 Chemical Structure

CAS No. 950762-95-5

Selleck's PCI-34051 has been cited by 39 publications

Purity & Quality Control

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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.
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
LAN1 M3G3Nmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHnuUZk4OiCqcoO= MVzHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDMRW4yKGOnbHzzJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OD1|LkpOwG0> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzFzNkG0O{c,OjNzMU[xOFc9N2F-
Jurkat M2PwVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUK3NkBpenN? NFTqPG1Iem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBLfXKtYYSgZ4VtdHNiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwQVEy|ryP NI\yNFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{GxOlE1Pyd-MkOxNVYyPDd:L3G+
NB-1 M{T6Omdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYDrdpJiPzJiaILz NYnsS4ZtT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVkJvMTDj[YxteyCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFNiYYPzZZktKEeLNUC9NVTPxE1? NWPwSVc1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOxNVYyPDdpPkKzNVE3OTR5PD;hQi=>
MT2 NYfQOVZuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVn4eXBOPzJiaILz NFvPdo1Iem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOXDJiY3XscJMhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgUXRUKGG|c3H5MEBIUTVyPUG1{txO M3nYUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MUG2NVQ4Lz5{M{GxOlE1PzxxYU6=
MT4 NHfV[nJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Moq3O|IhcHK| MXPHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNWFQh[2WubIOgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxRTJ3zszN M{jTVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MUG2NVQ4Lz5{M{GxOlE1PzxxYU6=
Huh7 M3fadWFvfGm4aYLhcEBie3OjeR?= NEfIfJA{KGSjeYO= NFXTVo5CdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJS1ZiZ3Xuc5R6eGViMXKgbY5n\WO2ZXSgbY4hcHWvYX6gTJVpPyClZXzsd{Bi\nSncjCzJIRigXNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVEvQM7:TR?= MnPyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2OUC3NFAoRjJ3NEmwO|AxRC:jPh?=
HuH7 NVn6cWI2S3m2b4TvfIlkcXS7IHHzd4F6 Mnn0N{Bl[Xm| NEHDU|VEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJfUh5IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDD2bYFjcWyrdImgZYZ1\XJiMzDkZZl{KGK7IFPlcIxVcXSncjC5OkBie3OjeTygR2M2OD1zMd88US=> NW\VXI5sRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0PVA4ODBpPkK1OFkxPzByPD;hQi=>
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SH-SY5Y M4qwWWN6fG:2b4jpZ4l1gSCjc4PhfS=> M4\hTGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNJNVO\NWmgZ4VtdHNiZYjwdoV{e2mwZzDUVFU{KGK7IFPlcIxVcXSnckm2JGFSfWWxdYOgc45mKHOxbIX0bY9vKGOnbHygdJJwdGmoZYLheIlwdiCjc4PhfS=> M17LclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEO1O|k3Lz5{OEizOVc6PjxxYU6=
IMR5 NGLBdm9EgXSxdH;4bYNqfHliYYPzZZk> NYThdZE{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUU2UNTDj[YxteyCneIDy[ZN{cW6pIGTQOVMh[nliQ3XscHRqfGW{OU[gRXF2\W:3czDvcoUhe2:udYTpc44h[2WubDDwdo9tcW[ncnH0bY9vKGG|c3H5 MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh|NUe5Okc,Ojh6M{W3PVY9N2F-
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Kelly NXS5TItNS3m2b4TvfIlkcXS7IHHzd4F6 NFG0fFhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBM\WyueTDj[YxteyCneIDy[ZN{cW6pIGTQOVMhdXW2YYTpc44h[nliQ3XscHRqfGW{OU[gRXF2\W:3czDvcoUhe2:udYTpc44h[2WubDDwdo9tcW[ncnH0bY9vKGG|c3H5 MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh|NUe5Okc,Ojh6M{W3PVY9N2F-
BE(2)-C NWLt[5VUS3m2b4TvfIlkcXS7IHHzd4F6 NVm3fWQyPzJiaILz M{jZNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJGMDJrLVOgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIJ6KG2nYYP1dolv\yCvZYThZo9tcWNiYXP0bZZqfHliYX\0[ZIhPzJiaILzJIJ6KFeVVD24JIF{e2G7LDDJR|UxRTF7LkpOwG0> NILIUFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG5NFA6Oid-MkmxPVAxQTJ:L3G+
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Sf9 MWXGeY5kfGmxbjDhd5NigQ>? MUK5NEBucW6| MX\Jcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKG[3bHygcIVv\3SqIFjERWM3KGW6cILld5Nm\CCrbjDmZYxtKGG{bYn3c5JuKFOoOTDj[YxteyC3c3nu[{BndHWxcn;n[Y5q[yCcTVHMJIF{KHO3YoP0doF1\SCjZoTldkA6OCCvaX7zJIJ6KG[udX;ybY1mfHKrYzDhcoFtgXOrczygTWM2OD12OD6y{txO MnLhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzOUCwPVIoRjJ7MUmwNFkzRC:jPh?=
BE(2)-C MlvGSpVv[3Srb36gZZN{[Xl? NWLRN25SPiC3TR?= MonTO|IhcHK| NUHTSHRwUW6qaXLpeIlwdiCxZjDISGFEQCCrbjDoeY1idiCERTiyLU1EKGOnbHzzJIF{e2W|c3XkJIF{KHWycnXneYxifGmxbjDv[kBxOjFxQ1TLUlEh\2WwZTDlfJBz\XO|aX;uJIF1KDZidV2gZYZ1\XJiN{KgbJJ{KGK7IGLUMXBEWiCjbnHsfZNqeyC{ZXzheIl3\SC2bzDjc451em:u MoLqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzOUCwPVIoRjJ7MUmwNFkzRC:jPh?=
BE(2)-C NVW1XWJmTnWwY4Tpc44h[XO|YYm= NEWyZ|k3KHWP NVPGfJRIPzJiaILz MnTkTY5pcWKrdHnvckBw\iCKRFHDPEBqdiCqdX3hckBDTSh{KT3DJINmdGy|IHHzd4V{e2WmIHHzJJVxemWpdXzheIlwdiCxZjDUdotCN06WUluxJIdmdmViZYjwdoV{e2mxbjDheEA3KHWPIHHmeIVzKDd{IHjyd{BjgSCUVD3QR3Ih[W6jbInzbZMhemWuYYTpeoUhfG9iY3;ueJJwdA>? NUjXNWxGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxPVAxQTJpPkK5NVkxODl{PD;hQi=>
BE(2)-C NVrMdGRTTnWwY4Tpc44h[XO|YYm= NW\F[Yt{PiC3TR?= NHjGRo84OiCqcoO= NYnMRmdmUW6qaXLpeIlwdiCxZjDISGFEQCCrbjDoeY1idiCERTiyLU1EKGOnbHzzJIF{e2W|c3XkJIF{KHWycnXneYxifGmxbjDv[kBVUCCpZX7lJIV5eHKnc4Ppc44h[XRiNjD1UUBi\nSncjC3NkBpenNiYomgVnQuWEOUIHHuZYx6e2m|IILlcIF1cX[nIITvJINwdnS{b3y= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF7MEC5Nkc,OjlzOUCwPVI9N2F-
BE(2)-C NIDnVFNHfW6ldHnvckBie3OjeR?= MnjPOkB2VQ>? NWjVeZdqPiCmYYnz MVjJcoR2[3Srb36gc4Yhd3W2Z4Lve5RpKG:oIH7leZJw\mmuYX3lcpQheG:|aYTpeoUhdmW3dILpeIUudGmtZTDzeJJ2[3S3cnXzJIlvKGi3bXHuJGJGMDJrLVOgZ4VtdHNiYYSgOkB2VSCjZoTldkA3KGSjeYOgZpkhTEGSST3zeIFqdmmwZzDiZZNm\CCvaXPyc5Nkd3CrYzDhcoFtgXOrcx?= NFzPdII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG5NFA6Oid-MkmxPVAxQTJ:L3G+
A673 NEnNPXhyUFSVIHHzd4F6 NF;ZSZZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= NXPrXJBTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC NWqyTXpueUiWUzDhd5NigQ>? MXXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB-EBc1 MlXMdWhVWyCjc4PhfS=> NF\vZ3RyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH M1HFPJFJXFNiYYPzZZk> MmXMdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO= M{HlTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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Assay
Methods Test Index PMID
Immunofluorescence SMC3 / Ac-SMC3 27072133

Protocol (from reference)

Kinase Assay:[1]
  • 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]
  • 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.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 296.32
Formula

C17H16N2O3

CAS No. 950762-95-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=CC=C(C=C1)CN2C=CC3=C2C=C(C=C3)C(=O)NO

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Handling Instructions

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