PCI-34051

Name: PCI-34051
Brand: Selleck Chemicals
SKU: S2012
Rating: 5 (38 reviews)

For research use only.

Catalog No.S2012

38 publications

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.

Selleck's PCI-34051 has been cited by 38 publications

Nat Biotechnol, 2015, 10.1038/nbt.3130

PubMed: 25751058 ( click the link to review the publication )

Thyroid, 2021, 10.1089/thy.2020.0948

PubMed: 34235979 ( click the link to review the publication )

Tuberculosis (Edinb), 2021, 127:102062

PubMed: 33639591 ( click the link to review the publication )

Nat Commun, 2020, 11(1):5783

PubMed: 33188197 ( click the link to review the publication )

Theranostics, 2020, 10(15):6790-6805

PubMed: 32550904 ( click the link to review the publication )

Cell Death Dis, 2020, 11(12):1036

PubMed: 33279948 ( click the link to review the publication )

FASEB J, 2020, 12

PubMed: 32281211 ( click the link to review the publication )

Int J Mol Sci, 2020, 21(12):E4539

PubMed: 32630606 ( click the link to review the publication )

Am J Transl Res, 2020, 12(10):6187-6203

PubMed: 33194023 ( click the link to review the publication )

EXCLI J, 2020, 19:734-744

PubMed: 32636726 ( click the link to review the publication )

Sci Rep, 2020, 10(1):12864

PubMed: 32733053 ( click the link to review the publication )

Theranostics, 2020, 10(16):7351-7368

PubMed: 32641996 ( click the link to review the publication )

Pathol Res Pract, 2020, 216(4):152867

PubMed: 32067803 ( click the link to review the publication )

Aging (Albany NY), 2020, 12(14):14174-14188

PubMed: 32692721 ( click the link to review the publication )

Cancer Res, 2019, 79(11):2947-2961

PubMed: 30987999 ( click the link to review the publication )

Cell Rep, 2019, 26(10):2608-2621.e6

PubMed: 30840885 ( click the link to review the publication )

Cancers (Basel), 2019, 11(5)E645

PubMed: 31083396 ( click the link to review the publication )

PLoS Genet, 2019, 15(2):e1007685

PubMed: 30779731 ( click the link to review the publication )

Biol Chem, 2019, 400(6):733-743

PubMed: 30521473 ( click the link to review the publication )

Nucl Med Biol, 2019, 74-75:1-11

PubMed: 31421440 ( click the link to review the publication )

Clin Hypertens, 2019, 25:13

PubMed: 31223486 ( click the link to review the publication )

Cancer Res, 2018, 78(20):5731-5740

PubMed: 30135193 ( click the link to review the publication )

J Med Chem, 2018, 61(22):10000-10016

PubMed: 30347148 ( click the link to review the publication )

Stem Cells Transl Med, 2018, 10.1002/sctm.18-0057

PubMed: 30426726 ( click the link to review the publication )
Oncol Rep, 2018, 40(2):635-646

PubMed: 29917168 ( click the link to review the publication )

Virol Sin, 2018, 33(5):418-428

PubMed: 30328580 ( click the link to review the publication )

Exp Mol Med, 2017, 49(2):e297

PubMed: 28232663 ( click the link to review the publication )

Chemistry, 2017, 23(13):3107-3116

PubMed: 27922200 ( click the link to review the publication )

Int J Mol Sci, 2017, 18(5)

PubMed: 28481295 ( click the link to review the publication )

PLoS One, 2017, 12(10):e0186620

PubMed: 29045501 ( click the link to review the publication )

ACS Chem Biol, 2016, 11(10):2685-2692

PubMed: 27459069 ( click the link to review the publication )

J Cell Mol Med, 2016, 20(12):2289-2298

PubMed: 27420561 ( click the link to review the publication )

Horm Cancer, 2016, 7(3):196-210

PubMed: 26957440 ( click the link to review the publication )

Nat Microbiol, 2016, 1:16174

PubMed: 27694949 ( click the link to review the publication )

J Immunol, 2015, 195(11):5421-31

PubMed: 26519528 ( click the link to review the publication )

Cancer Immunol Res, 2015, 3(12):1375-85

PubMed: 26297712 ( click the link to review the publication )

BMC Biol, 2014, 12:95

PubMed: 25406762 ( click the link to review the publication )

J Mol Biol, 2014, 426(20):3442-53

PubMed: 24657767 ( click the link to review the publication )

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description

Targets

HDAC8 ^[1]
(Cell-free assay)

10 nM

In vitro

PCI-34051 possesses promising potency for HDAC8 with a K_i 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	Activity Description	PMID
LAN1	MmnlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		Ml7TO\|IhcHK\|	MoDvS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUGFPOSClZXzsd{BqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO\|YYmsJGdKPTB;Mz65{txO	NVXQTo86RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOxNVYyPDdpPkKzNVE3OTR5PD;hQi=>
Jurkat	NEPzcYhIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		Ml:yO\|IhcHK\|	NE\kNpRIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBLfXKtYYSgZ4VtdHNiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwQVEy\|ryP	MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzFzNkG0O{c,OjNzMU[xOFc9N2F-
NB-1	NF72NndIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MVK3NkBpenN?	NFvpb21Iem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBPSi1zIHPlcIx{KGmwY4XiZZRm\CCob4KgO\|IhcHK\|IHL5JG1VWyCjc4PhfUwhT0l3ME2xOO69VQ>?	M3\hTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MUG2NVQ4Lz5{M{GxOlE1PzxxYU6=
MT2	M1nnZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		M4TpfVczKGi{cx?=	MULHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNWFIh[2WubIOgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxRTF3zszN	M3LF[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MUG2NVQ4Lz5{M{GxOlE1PzxxYU6=
MT4	NWjvPHlOT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		M3HZSlczKGi{cx?=	NGDmXGpIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOXDRiY3XscJMhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgUXRUKGG\|c3H5MEBIUTVyPUK1{txO	Mn3WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNzMU[xOFcoRjJ\|MUG2NVQ4RC:jPh?=
Huh7	NEPBOGJCdnSrdnnyZYwh[XO\|YYm=		M2n4V\|Mh\GG7cx?=	NV;RWVhkSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEOYIHflco91gXCnIEHiJIlv\mWldHXkJIlvKGi3bXHuJGh2cDdiY3XscJMh[W[2ZYKgN{Bl[Xm\|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0yNjkQvF2=	NGXtbYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS5NFcxOCd-MkW0PVA4ODB:L3G+
HuH7	NEDBNYhEgXSxdH;4bYNqfHliYYPzZZk>		M1ToblMh\GG7cx?=	NGHBd4NEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJfUh5IHPlcIx{KGG\|c3Xzd4VlKGG\|IHnubIljcXSrb36gc4Yh[2WubDD2bYFjcWyrdImgZYZ1\XJiMzDkZZl{KGK7IFPlcIxVcXSncjC5OkBie3OjeTygR2M2OD1zMd88US=>	Mn\yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2OUC3NFAoRjJ3NEmwO\|AxRC:jPh?=
Sf9	M{\VWmZ2dmO2aX;uJIF{e2G7		MnziOUBucW6\|	NYjXRWIzUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBnfWyuLXzlcod1cCCqdX3hckBENXSncn3pcoFtKE[OQVetTIl{NXSjZ3fl[EBJTEGFMTDlfJBz\XO\|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU3[5JIlve2WldDDj[YxteyC3c3nu[{BDd2NvTD3MfZMpSWNrLVHNR{BieyC\|dXLzeJJifGVicILlbY5kfWKjdHXkJIZweiB3IH3pcpMh\m:ubH;3[YQh[nlic4Xid5Rz[XSnIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDN3IH3pcpMh[nliZnz1c5Jme2OnLDDJR\|UxRTNwON88US=>	Moe0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6M{W3PVYoRjJ6OEO1O\|k3RC:jPh?=
Sf9	Mn20SpVv[3Srb36gZZN{[Xl?		M4TVZlUhdWmwcx?=	NU\6W5pLUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDmeYxtNWynbnf0bEBENXSncn3pcoFtKEircz30ZYdo\WRiSFTBR\|MhMDN7NTD0c{A1QDlicnXzbYR2\XNrL3j1cYFvKE6FT2KyJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6\|ZXP0JINmdGy\|IIXzbY5oKEKxYz3MMWx6eyiDYzmtRW1EKGG\|IIP1ZpN1emG2ZTDwdoV1emWjdHXkJIZweiB3IH3pcpMh\m:ubH;3[YQh[nlic4Xid5Rz[XSnIHHk[Il1cW:wIH3lZZN2emWmLDDJR\|UxRTdwMd88US=>	M1[5TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEO1O\|k3Lz5{OEizOVc6PjxxYU6=
Sf9	MnviSpVv[3Srb36gZZN{[Xl?		MlrXOUBucW6\|	MkC4TY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDoeY1idiCodXzsMYxmdme2aDDDMZRmem2rbnHsJGhqey22YXfn[YQhUESDQ{Kg[ZhxemW\|c3XkJIlvKGKjY4Xsc5ZqenW\|IHnu[oVkfGWmIGPmPUBqdnOnY4SgZ4VtdHNidYPpcochSm:lLVytUJl{MEGlKT3BUWMh[XNic4Xid5Rz[XSnIIDy[Ylv[3WkYYTl[EBnd3JiNTDtbY5{KG[xbHzve4VlKGK7IIP1ZpN1emG2ZTDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiB\|NTDtbY5{KGK7IH\seY9z\XOlZX7j[UBie3OjeTygTWM2OD1\|Md88US=>	M3zpOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEO1O\|k3Lz5{OEizOVc6PjxxYU6=
SH-SY5Y	NX7WdYxNS3m2b4TvfIlkcXS7IHHzd4F6			M4H2N2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNJNVO\NWmgZ4VtdHNiZYjwdoV{e2mwZzDUVFU{KGK7IFPlcIxVcXSnckm2JGFSfWWxdYOgc45mKHOxbIX0bY9vKGOnbHygdJJwdGmoZYLheIlwdiCjc4PhfS=>	NF3rcYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEizOVc6Pid-Mki4N\|U4QTZ:L3G+
IMR5	NF\xSopEgXSxdH;4bYNqfHliYYPzZZk>			MXPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDJUXI2KGOnbHzzJIV5eHKnc4PpcochXFB3MzDifUBE\WyuVHn0[ZI6PiCDUYXlc5V{KG:wZTDzc4x2fGmxbjDj[YxtKHC{b3zp[oVz[XSrb36gZZN{[Xl?	NETVeGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEizOVc6Pid-Mki4N\|U4QTZ:L3G+
SK-N-AS	MlLhR5l1d3SxeHnjbZR6KGG\|c3H5			Moq1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2suVi2DUzDj[YxteyCneIDy[ZN{cW6pIGTQOVMhdXW2YYTpc44h[nliQ3XscHRqfGW{OU[gRXF2\W:3czDvcoUhe2:udYTpc44h[2WubDDwdo9tcW[ncnH0bY9vKGG\|c3H5	MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh\|NUe5Okc,Ojh6M{W3PVY9N2F-
Kelly	NGXaPVVEgXSxdH;4bYNqfHliYYPzZZk>			NF75N25EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBM\WyueTDj[YxteyCneIDy[ZN{cW6pIGTQOVMhdXW2YYTpc44h[nliQ3XscHRqfGW{OU[gRXF2\W:3czDvcoUhe2:udYTpc44h[2WubDDwdo9tcW[ncnH0bY9vKGG\|c3H5	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh\|NUe5Okc,Ojh6M{W3PVY9N2F-
BE(2)-C	NHfW[llEgXSxdH;4bYNqfHliYYPzZZk>		Ml7rO\|IhcHK\|	MlnUR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRmUpOilvQzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgZpkhdWWjc4XybY5oKG2ndHHic4xq[yCjY4Tpeol1gSCjZoTldkA4OiCqcoOgZpkhX1OWLUigZZN{[XluIFnDOVA:OTlwOd88US=>	NEfPXpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG5NFA6Oid-MkmxPVAxQTJ:L3G+
Sf9	Mn:3SpVv[3Srb36gZZN{[Xl?		M3jsZlkxKG2rboO=	MlrMTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDoeY1idiCodXzsJIxmdme2aDDDMZRmem2rbnHsJGZNSUdvdHHn[4VlKEiGQVOxJIV5eHKnc4Pl[EBqdiCoYXzsJIFzdXm5b4LtJHNnQSClZXzsd{B2e2mwZzDmcJVwem:pZX7pZ{BbVUGOIHHzJJN2[nO2cnH0[UBi\nSncjC5NEBucW6\|IHL5JIZtfW:{aX3leJJq[yCjbnHsfZNqeyxiSVO1NF0zQC5\|zszN	MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF7MEC5Nkc,OjlzOUCwPVI9N2F-
Sf9	NF\V[5lHfW6ldHnvckBie3OjeR?=		NXn6S3ZvQTBibXnudy=>	M3HnNGlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iZoXscEBt\W6pdHigTGRCSzZiZYjwdoV{e2WmIHnuJIZidGxiYYLtfZdwem1iU3[5JINmdGy\|IIXzbY5oKG[udX;yc4dmdmmlIGrNRWwh[XNic4Xid5Rz[XSnIHHmeIVzKDlyIH3pcpMh[nliZnz1c5JqdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUS4MlLPxE1?	NELy[5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG5NFA6Oid-MkmxPVAxQTJ:L3G+
BE(2)-C	MoLKSpVv[3Srb36gZZN{[Xl?	NEPaRVk3KHWP	M4XBeVczKGi{cx?=	M1;aWGlvcGmkaYTpc44hd2ZiSFTBR\|ghcW5iaIXtZY4hSkVqMjmtR{Bk\WyuczDhd5Nme3OnZDDhd{B2eHKnZ4XsZZRqd25ib3[gdFIyN0OGS16xJIdmdmViZYjwdoV{e2mxbjDheEA3KHWPIHHmeIVzKDd{IHjyd{BjgSCUVD3QR3Ih[W6jbInzbZMhemWuYYTpeoUhfG9iY3;ueJJwdA>?	NFHjdpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG5NFA6Oid-MkmxPVAxQTJ:L3G+
BE(2)-C	MV\GeY5kfGmxbjDhd5NigQ>?	MoLiOkB2VQ>?	NG\oPGs4OiCqcoO=	M3PKWWlvcGmkaYTpc44hd2ZiSFTBR\|ghcW5iaIXtZY4hSkVqMjmtR{Bk\WyuczDhd5Nme3OnZDDhd{B2eHKnZ4XsZZRqd25ib3[gWJJsSS:QVGLLNUBo\W6nIHX4dJJme3Orb36gZZQhPiC3TTDh[pRmeiB5MjDodpMh[nliUmStVGNTKGGwYXz5d4l{KHKnbHH0bZZmKHSxIHPvcpRzd2x?	M1HEXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUmwNFkzLz5{OUG5NFA6OjxxYU6=
BE(2)-C	NX\YOIJFTnWwY4Tpc44h[XO\|YYm=	MknXOkB2VQ>?	NY\kUJE1PzJiaILz	MYPJcohq[mm2aX;uJI9nKEiGQVO4JIlvKGi3bXHuJGJGMDJrLVOgZ4VtdHNiYYPz[ZN{\WRiYYOgeZBz\We3bHH0bY9vKG:oIGTIJIdmdmViZYjwdoV{e2mxbjDheEA3KHWPIHHmeIVzKDd{IHjyd{BjgSCUVD3QR3Ih[W6jbInzbZMhemWuYYTpeoUhfG9iY3;ueJJwdA>?	NYj5[5pHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxPVAxQTJpPkK5NVkxODl{PD;hQi=>
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Sf9	M3rjPGZ2dmO2aX;uJIF{e2G7			M3TyNGlvcGmkaYTpc44hd2ZiTj30[ZJucW6jbDDHV3QufGGpZ3XkJIZ2dGxibHXu[5RpKGi3bXHuJGhFSUN4IHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCVZkmgbY5{\WO2IHPlcIx{KHW\|aX7nJHopSWNrTInzMWFOSyCjczDzeYJ{fHKjdHWgZpkh\my3b4LvcYV1emmlIH3leIhw\CxiSVO1NF01QC5{zszN	MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN2N{G0PEc,OzB\|NEexOFg9N2F-
Sf9	NVP5VWdHTnWwY4Tpc44h[XO\|YYm=		NIjUOXo1OCCvaX7z	NWfORZhKUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDmeYxtKGynbnf0bEBENXSncn3pcoFtKEircz30ZYdo\WRiSFTBR\|gh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJIlve2WldDDj[YxteyCvZXHzeZJm\CCjZoTldkA1OCCvaX7zJIJ6KEiGQVOtS4xwOS9{IHz1cYlv\XOlZX70JIF{e2G7LDDJR\|UxRTBwMEOxOlLPxE1?	NULGRYl[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OlQzQTBpPkOwPVY1OjlyPD;hQi=>
SK-N-BE(2)C	MlO2RY51cWOub37v[4VvcWNiYYPzZZk>		MofYPVYhcHK\|	MofXRY51cWOub37v[4VvcWNiYXP0bZZqfHliaX6gbJVu[W5iU1utUk1DTSh{KVOgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygdJJwdGmoZYLheIlwdiCrbnP1ZoF1\WRiZn;yJFk3KGi{czDifUBkenm\|dHHsJJZqd2yndDDzeIFqdmmwZzDiZZNm\CCjc4PhfUwhT0l3ME2xOe69VQ>?	Mkn0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF4M{CwOVQoRjNzNkOwNFU1RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Immunofluorescence	SMC3 / Ac-SMC3 ; PubMed: 27072133 J Biol Chem 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.	27072133

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]

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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)

References

[1] Balasubramanian S, et al. Leukemia. 2008, 22(5), 1026-1034.

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 Download PCI-34051 SDF

Molecular Weight	296.32
Formula	C₁₇H₁₆N₂O₃
CAS No.	950762-95-5
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
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)

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

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

Calculate Reset

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.

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.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

HDAC Signaling Pathway Map

HDAC Inhibitors with Unique Features

Pan HDAC Inhibitor

Panobinostat (LBH589) : Pan-HDAC inhibitor, IC50=5 nM.
Most Potent HDAC Inhibitor

Quisinostat (JNJ-26481585) : HDAC1, IC50=0.11 nM; HDAC2, IC50=0.33 nM.
FDA-approved HDAC Inhibitor

Vorinostat (SAHA, MK0683) : Approved by FDA against cutaneous T cell lymphoma.
Newest HDAC Inhibitor

RG2833 (RGFP109) ^New : Brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.

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Domatinostat (4SC-202) ^New

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Panobinostat (LBH589)

Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
Vorinostat (SAHA)

Vorinostat (suberoylanilide hydroxamic acid, SAHA, MK0683) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.
Entinostat (MS-275)

Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.
Trichostatin A (TSA)

Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays.
Romidepsin (FK228, Depsipeptide)

Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells.

Features:More effective than other classical HDAC inhibitors such as TSA, TPX, and butyrate.
Tubastatin A

Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.
Mocetinostat (MGCD0103)

Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.

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PCI-34051