Name: PCI-34051
Brand: Selleck Chemicals
SKU: S2012
Rating: 5 (39 reviews)

CAS No. 950762-95-5

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

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HDAC Signaling Pathway Map

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 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	Formulation	Activity Description	PMID

LAN1	NEDWZVZIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NYi4[XllPzJiaILz	NHHP[nJIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBNSU5zIHPlcIx{KGmwY4XiZZRm\CCob4KgO\|IhcHK\|IHL5JG1VWyCjc4PhfUwhT0l3ME2zMlnPxE1?	NYLYXml1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOxNVYyPDdpPkKzNVE3OTR5PD;hQi=>
Jurkat	NXfOUpdHT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NFyyNHg4OiCqcoO=	MlqxS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTpVzc2G2IHPlcIx{KGmwY4XiZZRm\CCob4KgO\|IhcHK\|IHL5JG1VWyCjc4PhfUwhT0l3ME2xNe69VQ>?	MmPpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNzMU[xOFcoRjJ\|MUG2NVQ4RC:jPh?=
NB-1	M3ztXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NFviTmM4OiCqcoO=	Mlv0S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUmIuOSClZXzsd{BqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO\|YYmsJGdKPTB;MUVOwG0>	M1;1RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MUG2NVQ4Lz5{M{GxOlE1PzxxYU6=
MT2	NGW2SWdIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NF\4SpU4OiCqcoO=	NWK2cY84T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVVR{IHPlcIx{KGmwY4XiZZRm\CCob4KgO\|IhcHK\|IHL5JG1VWyCjc4PhfUwhT0l3ME2xOe69VQ>?	NEPsfoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{GxOlE1Pyd-MkOxNVYyPDd:L3G+
MT4	Mn\aS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M1LnXlczKGi{cx?=	MmHhS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUXQ1KGOnbHzzJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OD1{Nd88US=>	M13nblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MUG2NVQ4Lz5{M{GxOlE1PzxxYU6=
Huh7	MoHmRY51cX[rcnHsJIF{e2G7		MmnON{Bl[Xm\|	NHPRNZdCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJS1ZiZ3Xuc5R6eGViMXKgbY5n\WO2ZXSgbY4hcHWvYX6gTJVpPyClZXzsd{Bi\nSncjCzJIRigXNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVEvQM7:TR?=	NGHONmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS5NFcxOCd-MkW0PVA4ODB:L3G+
HuH7	M1Xk[2N6fG:2b4jpZ4l1gSCjc4PhfS=>		NG\icms{KGSjeYO=	MYfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIeWg4KGOnbHzzJIF{e2W\|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCC4aXHibYxqfHliYX\0[ZIhOyCmYYnzJIJ6KEOnbHzUbZRmeiB7NjDhd5NigSxiQ1O1NF0yOc7:TR?=	MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR7MEewNEc,OjV2OUC3NFA9N2F-
Sf9	NYqzeXhqTnWwY4Tpc44h[XO\|YYm=		NVr2VmkzPSCvaX7z	M3LQ[GlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSg[pVtdC2uZX7neIghcHWvYX6gR{11\XKvaX7hcEBHVEGJLVjpd{11[WepZXSgTGRCSzFiZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{KGmwZnXjeIVlKFOoOTDpcpNm[3RiY3XscJMhfXOrbnegRo9kNUxvTInzLGFkMS2DTVOgZZMhe3Wkc4TyZZRmKHC{ZXnuZ5Vj[XSnZDDmc5IhPSCvaX7zJIZwdGyxd3XkJIJ6KHO3YoP0doF1\SCjZHTpeIlwdiCvZXHzeZJm\CCjZoTldkA{PSCvaX7zJIJ6KG[udX;y[ZNk\SxiSVO1NF0{NjkQvF2=	MmPwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6M{W3PVYoRjJ6OEO1O\|k3RC:jPh?=
Sf9	NXHTZ\|NMTnWwY4Tpc44h[XO\|YYm=		M2iwflUhdWmwcx?=	M{f1bGlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iZoXscE1t\W6pdHigR{11\XKvaX7hcEBJcXNvdHHn[4VlKEiGQVOzJEg{QTVidH:gOFg6KHKnc3nkeYV{MS:qdX3hckBPS0:UMjDlfJBz\XO\|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU3[5JIlve2WldDDj[YxteyC3c3nu[{BDd2NvTD3MfZMpSWNrLVHNR{BieyC\|dXLzeJJifGVicILleJJm[XSnZDDmc5IhPSCvaX7zJIZwdGyxd3XkJIJ6KHO3YoP0doF1\SCjZHTpeIlwdiCvZXHzeZJm\CxiSVO1NF04NjIQvF2=	M2PIUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEO1O\|k3Lz5{OEizOVc6PjxxYU6=
Sf9	MXHGeY5kfGmxbjDhd5NigQ>?		NET2XWg2KG2rboO=	MUXJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKG[3bHytcIVv\3SqIFOteIVzdWmwYXygTIl{NXSjZ3fl[EBJTEGFMjDlfJBz\XO\|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU3[5JIlve2WldDDj[YxteyC3c3nu[{BDd2NvTD3MfZMpSWNrLVHNR{BieyC\|dXLzeJJifGVicILlbY5kfWKjdHXkJIZweiB3IH3pcpMh\m:ubH;3[YQh[nlic4Xid5Rz[XSnIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDN3IH3pcpMh[nliZnz1c5Jme2OnbnPlJIF{e2G7LDDJR\|UxRTNzzszN	NYfrdJR1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4N\|U4QTZpPkK4PFM2Pzl4PD;hQi=>
SH-SY5Y	M3PXRmN6fG:2b4jpZ4l1gSCjc4PhfS=>			M3nUcWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNJNVO\NWmgZ4VtdHNiZYjwdoV{e2mwZzDUVFU{KGK7IFPlcIxVcXSnckm2JGFSfWWxdYOgc45mKHOxbIX0bY9vKGOnbHygdJJwdGmoZYLheIlwdiCjc4PhfS=>	MnTzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6M{W3PVYoRjJ6OEO1O\|k3RC:jPh?=
IMR5	NFrHToVEgXSxdH;4bYNqfHliYYPzZZk>			NWPTXIdFS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUU2UNTDj[YxteyCneIDy[ZN{cW6pIGTQOVMh[nliQ3XscHRqfGW{OU[gRXF2\W:3czDvcoUhe2:udYTpc44h[2WubDDwdo9tcW[ncnH0bY9vKGG\|c3H5	NXv6cm9QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4N\|U4QTZpPkK4PFM2Pzl4PD;hQi=>
SK-N-AS	NHL1PGtEgXSxdH;4bYNqfHliYYPzZZk>			NVPGWHZsS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvTj3BV{Bk\WyuczDlfJBz\XO\|aX7nJHRRPTNibYX0ZZRqd25iYomgR4VtdFSrdHXyPVYhSVG3ZX;1d{BwdmVic3;seZRqd25iY3XscEBxem:uaX\ldoF1cW:wIHHzd4F6	M4f6[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEO1O\|k3Lz5{OEizOVc6PjxxYU6=
Kelly	NEe5PI9EgXSxdH;4bYNqfHliYYPzZZk>			MnLTR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT4VtdHliY3XscJMh\XiycnXzd4lv\yCWUEWzJI12fGG2aX;uJIJ6KEOnbHzUbZRmejl4IFHReYVwfXNib37lJJNwdHW2aX;uJINmdGxicILvcIln\XKjdHnvckBie3OjeR?=	NXLDdplPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4N\|U4QTZpPkK4PFM2Pzl4PD;hQi=>
BE(2)-C	NFrSWG1EgXSxdH;4bYNqfHliYYPzZZk>		MkHkO\|IhcHK\|	MX3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCSUgzMS2FIHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDifUBu\WG\|dYLpcochdWW2YXLvcIlkKGGldHn2bZR6KGGodHXyJFczKGi{czDifUBYW1RvODDhd5NigSxiSVO1NF0yQS57zszN	NUO1VHJrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxPVAxQTJpPkK5NVkxODl{PD;hQi=>
Sf9	Ml[ySpVv[3Srb36gZZN{[Xl?		NUL4dmx2QTBibXnudy=>	NGj0TndKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIh2dWGwIH\1cIwhdGWwZ4ToJGMufGW{bXnuZYwhTkyDRz30ZYdo\WRiSFTBR\|Eh\XiycnXzd4VlKGmwIH\hcIwh[XKveYfvdo0hW2Z7IHPlcIx{KHW\|aX7nJIZtfW:{b3flcolkKFqPQVygZZMhe3Wkc4TyZZRmKGGodHXyJFkxKG2rboOgZpkh\my3b4LpcYV1emmlIHHuZYx6e2m\|LDDJR\|UxRTJ6LkROwG0>	MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF7MEC5Nkc,OjlzOUCwPVI9N2F-
Sf9	Mnn1SpVv[3Srb36gZZN{[Xl?		M4Xv[\|kxKG2rboO=	MWLJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKG[3bHygcIVv\3SqIFjERWM3KGW6cILld5Nm\CCrbjDmZYxtKGG{bYn3c5JuKFOoOTDj[YxteyC3c3nu[{BndHWxcn;n[Y5q[yCcTVHMJIF{KHO3YoP0doF1\SCjZoTldkA6OCCvaX7zJIJ6KG[udX;ybY1mfHKrYzDhcoFtgXOrczygTWM2OD12OD6y{txO	MoP6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzOUCwPVIoRjJ7MUmwNFkzRC:jPh?=
BE(2)-C	MlXESpVv[3Srb36gZZN{[Xl?	M2LwVVYhfU1?	MX[3NkBpenN?	NIKyVnVKdmirYnn0bY9vKG:oIFjERWM5KGmwIHj1cYFvKEKHKEKpMWMh[2WubIOgZZN{\XO\|ZXSgZZMhfXC{ZXf1cIF1cW:wIH;mJJAzOS:FRFvONUBo\W6nIHX4dJJme3Orb36gZZQhPiC3TTDh[pRmeiB5MjDodpMh[nliUmStVGNTKGGwYXz5d4l{KHKnbHH0bZZmKHSxIHPvcpRzd2x?	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF7MEC5Nkc,OjlzOUCwPVI9N2F-
BE(2)-C	NXHHc\|A{TnWwY4Tpc44h[XO\|YYm=	MUK2JJVO	NWL4cY9uPzJiaILz	MlOwTY5pcWKrdHnvckBw\iCKRFHDPEBqdiCqdX3hckBDTSh{KT3DJINmdGy\|IHHzd4V{e2WmIHHzJJVxemWpdXzheIlwdiCxZjDUdotCN06WUluxJIdmdmViZYjwdoV{e2mxbjDheEA3KHWPIHHmeIVzKDd{IHjyd{BjgSCUVD3QR3Ih[W6jbInzbZMhemWuYYTpeoUhfG9iY3;ueJJwdA>?	MmXGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzOUCwPVIoRjJ7MUmwNFkzRC:jPh?=
BE(2)-C	NX;IXIN6TnWwY4Tpc44h[XO\|YYm=	NFLPeXY3KHWP	MUC3NkBpenN?	NVLENYdtUW6qaXLpeIlwdiCxZjDISGFEQCCrbjDoeY1idiCERTiyLU1EKGOnbHzzJIF{e2W\|c3XkJIF{KHWycnXneYxifGmxbjDv[kBVUCCpZX7lJIV5eHKnc4Ppc44h[XRiNjD1UUBi\nSncjC3NkBpenNiYomgVnQuWEOUIHHuZYx6e2m\|IILlcIF1cX[nIITvJINwdnS{b3y=	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF7MEC5Nkc,OjlzOUCwPVI9N2F-
BE(2)-C	M321WWZ2dmO2aX;uJIF{e2G7	NFi1cGY3KHWP	MlnuOkBl[Xm\|	MYPJcoR2[3Srb36gc4Yhd3W2Z4Lve5RpKG:oIH7leZJw\mmuYX3lcpQheG:\|aYTpeoUhdmW3dILpeIUudGmtZTDzeJJ2[3S3cnXzJIlvKGi3bXHuJGJGMDJrLVOgZ4VtdHNiYYSgOkB2VSCjZoTldkA3KGSjeYOgZpkhTEGSST3zeIFqdmmwZzDiZZNm\CCvaXPyc5Nkd3CrYzDhcoFtgXOrcx?=	NEGx[ZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG5NFA6Oid-MkmxPVAxQTJ:L3G+
A673	NVnyNWFoeUiWUzDhd5NigQ>?			M1TXOZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy\|	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SK-N-MC	M{LSZpFJXFNiYYPzZZk>			NWnuU5RTeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM>	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
NB-EBc1	NX3E[IFteUiWUzDhd5NigQ>?			MnuydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6ELVXCZ\|Eh[2WubIO=	NI\pZ2U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
SK-N-SH	MYPxTHRUKGG\|c3H5			NWDqXlFkeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM>	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
NB1643	MmK4dWhVWyCjc4PhfS=>			MnTzdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?=	MmWwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
LAN-5	M4TwcZFJXFNiYYPzZZk>			M4nsOZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?=	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Jurkat	M2P5TWFvfGmycn;sbYZmemG2aY\lJIF{e2G7			NF[2WFFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFr1dotifCClZXzsd{BjgSCjbHHtZZIh[my3ZTDhd5NigSxiR1m1NF0zNjUQvF2=	NHTSOXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWwOVk{PSd-Mkm1NFU6OzV:L3G+
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Sf9	NFG2fGpHfW6ldHnvckBie3OjeR?=			MYnJcohq[mm2aX;uJI9nKENvdHXycYlv[WxiRlzBS{9JcXNvdHHn[4VlKG[3bHygcIVv\3SqIHj1cYFvKEiGQVOxJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6\|ZXP0JINmdGy\|IIXzbY5oKFpqQXOpUJl{NUGPQzDhd{B{fWK\|dILheIUh[nliZnz1c5JwdWW2cnnjJI1mfGixZDygTWM2OD1{OD6z{txO	NETodZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEO0O\|E1QCd-M{CzOFcyPDh:L3G+
Sf9	NVzjb2k3TnWwY4Tpc44h[XO\|YYm=			MV\Jcohq[mm2aX;uJI9nKE5vdHXycYlv[WxiR2PUMZRi\2enZDDmeYxtKGynbnf0bEBpfW2jbjDISGFEPiCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDaLGFkMUy7cz3BUWMh[XNic4Xid5Rz[XSnIHL5JIZtfW:{b33leJJq[yCvZYToc4QtKEmFNUC9OFgvOs7:TR?=	MmryQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB\|NEexOFgoRjNyM{S3NVQ5RC:jPh?=
Sf9	Mn;ISpVv[3Srb36gZZN{[Xl?		NIKxb4Y1OCCvaX7z	MnrhTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDoeY1idiCodXzsJIxmdme2aDDDMZRmem2rbnHsJGhqey22YXfn[YQhUESDQ{ig[ZhxemW\|c3XkJIlvKGKjY4Xsc5ZqenW\|IHnu[oVkfGWmIHnud4VkfCClZXzsd{Bu\WG\|dYLl[EBi\nSncjC0NEBucW6\|IHL5JGhFSUNvR3zvNU8zKGy3bXnu[ZNk\W62IHHzd4F6NCCLQ{WwQVAvODNzNkNOwG0>	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl4NEK5NEc,OzB7NkSyPVA9N2F-
SK-N-BE(2)C	M1XrRmFvfGmlbH;uc4dmdmmlIHHzd4F6		M13qOVk3KGi{cx?=	NH73RoZCdnSrY3zvco9o\W6rYzDhZ5Rqfmm2eTDpckBpfW2jbjDTT{1PNUKHKEKpR{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEBxem:uaX\ldoF1cW:wIHnuZ5Vj[XSnZDDmc5IhQTZiaILzJIJ6KGO{eYP0ZYwhfmmxbHX0JJN1[WmwaX7nJIJie2WmIHHzd4F6NCCJSUWwQVE2\|ryP	NIPDcms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MU[zNFA2PCd-M{G2N\|AxPTR:L3G+

Click to View More Cell Line Experimental Data

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.
(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. Click to purchase: PEG300 Tween 80	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
Formula	C₁₇H₁₆N₂O₃
CAS No.	950762-95-5
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	COC1=CC=C(C=C1)CN2C=CC3=C2C=C(C=C3)C(=O)NO

Download PCI-34051 SDF

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: g Dosing volume per animal:μL 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

%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

Dilution Calculator Molecular Weight 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

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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):