PCI-34051

製品コード：S2012 純度：99.79%

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.

CAS No. 950762-95-5

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 33000	国内在庫あり
10mg	JPY 25500	国内在庫あり
1g	JPY 448500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（48）

製品安全説明書

現在のバッチを見る：純度： 99.79%

99.79

PCI-34051関連製品

関連ターゲット	HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2	もっと見る
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関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	もっと見る

シグナル伝達経路

HDACシグナル伝達経路

HDAC阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
BE(2)-C	Function assay	6 uM	72 hrs	Inhibition of HDAC8 in human BE(2)-C cells assessed as upregulation of p21/CDKN1 gene expression at 6 uM after 72 hrs by RT-PCR analysis relative to control	29190092
BE(2)-C	Function assay	6 uM	72 hrs	Inhibition of HDAC8 in human BE(2)-C cells assessed as upregulation of TrkA/NTRK1 gene expression at 6 uM after 72 hrs by RT-PCR analysis relative to control	29190092
BE(2)-C	Function assay	6 uM	72 hrs	Inhibition of HDAC8 in human BE(2)-C cells assessed as upregulation of TH gene expression at 6 uM after 72 hrs by RT-PCR analysis relative to control	29190092
BE(2)-C	Function assay	6 uM	6 days	Induction of outgrowth of neurofilament positive neutrite-like structures in human BE(2)-C cells at 6 uM after 6 days by DAPI-staining based microscopic analysis	29190092
MT2	Growth inhibition assay		72 hrs	Growth inhibition of human MT2 cells incubated for 72 hrs by MTS assay, GI50=15μM	23116147
NB-1	Growth inhibition assay		72 hrs	Growth inhibition of human NB-1 cells incubated for 72 hrs by MTS assay, GI50=14μM	23116147
Jurkat	Growth inhibition assay		72 hrs	Growth inhibition of human Jurkat cells incubated for 72 hrs by MTS assay, GI50=11μM	23116147
LAN1	Growth inhibition assay		72 hrs	Growth inhibition of human LAN1 cells incubated for 72 hrs by MTS assay, GI50=3.9μM	23116147
MT4	Growth inhibition assay		72 hrs	Growth inhibition of human MT4 cells incubated for 72 hrs by MTS assay, GI50=25μM	23116147
Huh7	Antiviral assay		3 days	Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay, EC50=1.8μM	25490700
HuH7	Cytotoxicity assay		3 days	Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay, CC50=11μM	25490700
Sf9	Function assay		5 mins	Inhibition of recombinant full-length human C-terminal FLAG-His-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using Boc-L-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 35 mins by fluoresce, IC50=3.8μM	28835796
Sf9	Function assay		5 mins	Inhibition of recombinant human full-length C-terminal His-tagged HDAC3 (395 to 489 residues)/human NCOR2 expressed in baculovirus infected Sf9 insect cells using Boc-L-Lys(Ac)-AMC as substrate pretreated for 5 mins followed by substrate addition measured, IC50=7.1μM	28835796
Sf9	Function assay		5 mins	Inhibition of recombinant human full-length C-terminal His-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells using Boc-L-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 35 mins by fluorescence assay, IC50=31μM	28835796
BE(2)-C	Cytotoxicity assay		72 hrs	Cytotoxicity against human BE(2)-C cells assessed as reduction in cell viability by measuring metabolic activity after 72 hrs by WST-8 assay, IC50=19.9μM	29190092
Sf9	Function assay		90 mins	Inhibition of recombinant human full length C-terminal FLAG-tagged HDAC1 expressed in fall armyworm Sf9 cells using fluorogenic ZMAL as substrate after 90 mins by fluorimetric analysis, IC50=28.3μM	29190092
Sf9	Function assay		90 mins	Inhibition of recombinant human full length HDAC6 expressed in fall armyworm Sf9 cells using fluorogenic ZMAL as substrate after 90 mins by fluorimetric analysis, IC50=48.2μM	29190092
Jurkat	Antiproliferative assay		48 hrs	Antiproliferative activity against human Jurkat cells after 48 hrs by MTT assay, IC50=4.5μM	29533873
MOLT4	Antiproliferative assay		48 hrs	Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay, IC50=9.4μM	29533873
HEL	Antiproliferative assay		48 hrs	Antiproliferative activity against human HEL cells after 48 hrs by MTT assay, IC50=10.8μM	29533873
SK-N-BE(2)	Antiproliferative assay		48 hrs	Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay, IC50=16.9μM	29533873
PC3	Antiproliferative assay		48 hrs	Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50=19.2μM	29533873
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells after 72 hrs by MTS assay, GI50=2.01μM	30004697
K562R	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562R cells after 72 hrs by MTS assay, GI50=2.2μM	30004697
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, GI50=2.64μM	30004697
PC3	Antiproliferative assay		72 hrs	Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay, GI50=2.66μM	30004697
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay, GI50=2.97μM	30004697
Sf9	Function assay		40 mins	Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected insect cells measured after 40 mins by HDAC-Glo1/2 luminescent assay, IC50=0.03162μM	30964290
SK-N-BE(2)C	Anticlonogenic assay		96 hrs	Anticlonogenic activity in human SK-N-BE(2)C cells assessed as reduction in cell proliferation incubated for 96 hrs by crystal violet staining based assay, GI50=15μM	31630054
SH-SY5Y	Cytotoxicity assay			Cytotoxicity against human SH-SY5Y cells expressing TP53 by CellTiter96 AQueous one solution cell proliferation assay	28835796
IMR5	Cytotoxicity assay			Cytotoxicity against human IMR5 cells expressing TP53 by CellTiter96 AQueous one solution cell proliferation assay	28835796
SK-N-AS	Cytotoxicity assay			Cytotoxicity against human SK-N-AS cells expressing TP53 mutation by CellTiter96 AQueous one solution cell proliferation assay	28835796
Kelly	Cytotoxicity assay			Cytotoxicity against human Kelly cells expressing TP53 mutation by CellTiter96 AQueous one solution cell proliferation assay	28835796
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Jurkat	Antiproliferative assay			Antiproliferative activity against human Jurkat cells by alamar blue assay, GI50=2.4μM	29505935
HUT78	Antiproliferative assay			Antiproliferative activity against human HUT78 cells by alamar blue assay, GI50=2.4μM	29505935
HSB2	Antiproliferative assay			Antiproliferative activity against human HSB2 cells by alamar blue assay, GI50=2.4μM	29505935
MOLT4	Antiproliferative assay			Antiproliferative activity against human MOLT4 cells by alamar blue assay, GI50=2.4μM	29505935
BL21 (DE3)	Function assay			Binding affinity to human His-thioredoxin-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells by ITC method, Kd=0.0751μM	30347148
BL21 (DE3)	Function assay			Inhibition of human His-thioredoxin-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method, IC50=0.0777μM	30347148
BL21 (DE3)	Function assay			Binding affinity to Schistosoma mansoni His-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells by ITC method, Kd=0.367μM	30347148
BL21 (DE3)	Function assay			Inhibition of Schistosoma mansoni His-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method, IC50=0.4358μM	30347148
BL21 (DE3)	Function assay			Inhibition of human His-thioredoxin-tagged HDAC8 mL6/L179I mutant expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method, IC50=1μM	30347148
BL21 (DE3)	Function assay			Inhibition of human His-thioredoxin-tagged HDAC8 mL6 mutant expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method, IC50=1.63μM	30347148
BL21 (DE3)	Function assay			Inhibition of human His-thioredoxin-tagged HDAC8 mL1/mL6 mutant expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method, IC50=2.7μM	30347148
BL21 (DE3)	Function assay			Inhibition of human His-thioredoxin-tagged HDAC8 mL1/mL6/L179I mutant expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method, IC50=5μM	30347148
Sf9	Function assay			Inhibition of C-terminal FLAG/His-tagged full length human HDAC1 expressed in baculovirus infected Sf9 insect cells using Z(Ac)Lys-AMC as substrate by fluorometric method, IC50=28.3μM	30347148
Sf9	Function assay			Inhibition of N-terminal GST-tagged full length human HDAC6 expressed in baculovirus infected Sf9 insect cells using Z(Ac)Lys-AMC as substrate by fluorometric method, IC50=48.2μM	30347148
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生物活性

製品説明

Targets

HDAC8 ^[1]
(Cell-free assay)

10 nM

In Vitro
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]
Kinase Assay	Histone deacetylase activity
Kinase Assay	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.
細胞実験	細胞株	A549 cell line, Ovcar-3 cell line
	濃度	5 μM
	反応時間	24 hours
	実験の流れ	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.
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Immunofluorescence	SMC3 / Ac-SMC3		27072133

In Vivo
In Vivo	PCI-34051 is a potent and specific HDAC8 inhibitor.
動物実験	動物モデル	Male C57BL/6 and BALB/c mice
	投与量	40 mg/kg
	投与経路	i.p.

参考
[1] Balasubramanian S, et al. Leukemia. 2008, 22(5), 1026-1034. [2] Zhou W, et al. Theranostics. 2020 May 21;10(15):6790-6805.

参考

化学情報

分子量	296.32	化学式	C₁₇H₁₆N₂O₃
CAS No.	950762-95-5	SDF	Download PCI-34051 SDFをダウンロードする
Smiles	COC1=CC=C(C=C1)CN2C=CC3=C2C=C(C=C3)C(=O)NO
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 59 mg/mL ( (199.1 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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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):