Art. -Nr.: HY-15224

PCI-34051

31 Cited Publications

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Based on 31 publication(s) in Google Scholar

PCI-34051 is a potent and selective HDAC8 inhibitor with IC₅₀ of 10 nM, with >200-fold selectivity over the other HDAC isoforms.

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Reinheit: 99.84%
CAS. Nr.: 950762-95-5
Formel: C₁₇H₁₆N₂O₃
Molecular Weight:296.32

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PCI-34051 Chemical Structure

CAS. Nr.: 950762-95-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (31)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
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Bioz

Biologische Aktivität

Beschreibung

PCI-34051 is a potent and selective HDAC8 inhibitor with IC₅₀ of 10 nM, with >200-fold selectivity over the other HDAC isoforms.

IC₅₀ & Target^[1]

HDAC8

10 nM (IC₅₀)

HDAC6

2.9 μM (IC₅₀)

HDAC1

4 μM (IC₅₀)

HDAC10

13 μM (IC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	19 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human A549 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human A549 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
A549	GI₅₀	>20000 nM Compound: PCI-34051	Antiproliferative activity against human A549 cells after 72 hrs by MTS assay Antiproliferative activity against human A549 cells after 72 hrs by MTS assay	[PMID: 30004697]
A549	IC₅₀	2 μM Compound: PCI-34051	Antiproliferative activity against human A549 cells after 72 hrs by CellTiter Glo assay Antiproliferative activity against human A549 cells after 72 hrs by CellTiter Glo assay	[PMID: 35797900]
A549	IC₅₀	13.11 μM Compound: 1; PCI-34051	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs under irradiation by CCK-8 method Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs under irradiation by CCK-8 method	[PMID: 36516047]
A549	IC₅₀	15.84 μM Compound: 1; PCI-34051	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 method Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 method	[PMID: 36516047]
A549	GI₅₀	15.84 μM Compound: PCI-34051	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 48 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 48 hrs by SRB assay	[PMID: 37607440]
A549	IC₅₀	>33.3 μM Compound: PCI-34051	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 39089850]
BE(2)-C	IC₅₀	19.9 μM Compound: 1; PCI-34051	Cytotoxicity against human BE(2)-C cells assessed as reduction in cell viability by measuring metabolic activity after 72 hrs by WST-8 assay Cytotoxicity against human BE(2)-C cells assessed as reduction in cell viability by measuring metabolic activity after 72 hrs by WST-8 assay	[PMID: 29190092]
BE(2)-C	IC₅₀	3.1 μM Compound: PCI34051	Inhibition of colony formation in human BE(2)-C cells Inhibition of colony formation in human BE(2)-C cells	[PMID: 32672458]
BXPC-3	GI₅₀	>20000 nM Compound: PCI-34051	Antiproliferative activity against human BxPC3 cells after 72 hrs by MTS assay Antiproliferative activity against human BxPC3 cells after 72 hrs by MTS assay	[PMID: 30004697]
CCRF-HSB-2	GI₅₀	1.4 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human CCRF-HSB-2 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human CCRF-HSB-2 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
CCRF-HSB-2	GI₅₀	2.4 μM Compound: 41; PCI-34051	Antiproliferative activity against human HSB2 cells by alamar blue assay Antiproliferative activity against human HSB2 cells by alamar blue assay	[PMID: 29505935]
DB	GI₅₀	21.2 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human DB cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human DB cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
DOHH-2	IC₅₀	3.14 μM Compound: PCI-34051	Antiproliferative activity against human DOHH-2 cells assessed as cell viability measured after 72 hrs by Alamar Blue Assay Antiproliferative activity against human DOHH-2 cells assessed as cell viability measured after 72 hrs by Alamar Blue Assay	[PMID: 38949959]
HCT-116	GI₅₀	>20 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human HCT-116 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human HCT-116 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
HCT-116	GI₅₀	2640 nM Compound: PCI-34051	Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay	[PMID: 30004697]
HCT-116	GI₅₀	2600 nM Compound: PCI-34051	Antiproliferative activity against human HCT-116 cells after 72 hrs by CellTiter Glo assay Antiproliferative activity against human HCT-116 cells after 72 hrs by CellTiter Glo assay	[PMID: 35797900]
HCT-116	IC₅₀	21.9 μM Compound: PCI-34051	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 39089850]
HEL	IC₅₀	10.8 μM Compound: 1; PCI-34051	Antiproliferative activity against human HEL cells after 48 hrs by MTT assay Antiproliferative activity against human HEL cells after 48 hrs by MTT assay	[PMID: 29533873]
HeLa	GI₅₀	>20 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human HeLa cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human HeLa cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
HeLa	IC₅₀	>100 μM Compound: 6, PCI-34051	Inhibition of HDAC in human HeLa cells nuclear extracts by fluorometric assay Inhibition of HDAC in human HeLa cells nuclear extracts by fluorometric assay	[PMID: 23116147]
HeLa	IC₅₀	>25 μM Compound: 1; PCI-34051	Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay	[PMID: 29533873]
HH	GI₅₀	>100 μM Compound: 6, PCI-34051	Growth inhibition of human HH cells incubated for 72 hrs by MTS assay Growth inhibition of human HH cells incubated for 72 hrs by MTS assay	[PMID: 23116147]
HT-29	GI₅₀	>10000 nM Compound: PCI-34051	Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay	[PMID: 30004697]
HT-29	IC₅₀	>10000 nM Compound: PCI-34051	Antiproliferative activity against human HT-29 cells after 72 hrs by CellTiter Glo assay Antiproliferative activity against human HT-29 cells after 72 hrs by CellTiter Glo assay	[PMID: 35797900]
Huh-7	CC₅₀	11 μM Compound: 10, PCI-34051	Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay	[PMID: 25490700]
Huh-7	EC₅₀	1.8 μM Compound: 10, PCI-34051	Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay	[PMID: 25490700]
HuT78	GI₅₀	4 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human HuT78 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human HuT78 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
HuT78	GI₅₀	2.4 μM Compound: 41; PCI-34051	Antiproliferative activity against human HUT78 cells by alamar blue assay Antiproliferative activity against human HUT78 cells by alamar blue assay	[PMID: 29505935]
Jurkat	GI₅₀	2.4 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human Jurkat cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human Jurkat cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
Jurkat	GI₅₀	11 μM Compound: 6, PCI-34051	Growth inhibition of human Jurkat cells incubated for 72 hrs by MTS assay Growth inhibition of human Jurkat cells incubated for 72 hrs by MTS assay	[PMID: 23116147]
Jurkat	GI₅₀	2.4 μM Compound: 41; PCI-34051	Antiproliferative activity against human Jurkat cells by alamar blue assay Antiproliferative activity against human Jurkat cells by alamar blue assay	[PMID: 29505935]
Jurkat	IC₅₀	4.5 μM Compound: 1; PCI-34051	Antiproliferative activity against human Jurkat cells after 48 hrs by MTT assay Antiproliferative activity against human Jurkat cells after 48 hrs by MTT assay	[PMID: 29533873]
Jurkat	GI₅₀	2.4 μM Compound: 7; PCI-34051	Growth inhibition of human Jurkat cells Growth inhibition of human Jurkat cells	[PMID: 37429084]
Jurkat	IC₅₀	4.5 μM Compound: PCI-34051	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 39089850]
K562	GI₅₀	33.6 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human K562 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human K562 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
K562	IC₅₀	>25 μM Compound: 1; PCI-34051	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 29533873]
K562	GI₅₀	2010 nM Compound: PCI-34051	Antiproliferative activity against human K562 cells after 72 hrs by MTS assay Antiproliferative activity against human K562 cells after 72 hrs by MTS assay	[PMID: 30004697]
K562	IC₅₀	2010 nM Compound: PCI-34051	Antiproliferative activity against human K562 cells after 72 hrs by CellTiter Glo assay Antiproliferative activity against human K562 cells after 72 hrs by CellTiter Glo assay	[PMID: 35797900]
K562	IC₅₀	2200 nM Compound: PCI-34051	Antiproliferative activity against imatinib-resistant human K562 cells over expressing MDR1 after 72 hrs by CellTiter Glo assay Antiproliferative activity against imatinib-resistant human K562 cells over expressing MDR1 after 72 hrs by CellTiter Glo assay	[PMID: 35797900]
K-562R	GI₅₀	2200 nM Compound: PCI-34051	Antiproliferative activity against human K562R cells after 72 hrs by MTS assay Antiproliferative activity against human K562R cells after 72 hrs by MTS assay	[PMID: 30004697]
MCF7	GI₅₀	>20 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human MCF7 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human MCF7 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
MCF7	GI₅₀	2970 nM Compound: PCI-34051	Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay	[PMID: 30004697]
MCF7	IC₅₀	2980 nM Compound: PCI-34051	Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter Glo assay Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter Glo assay	[PMID: 35797900]
MDA-MB-231	IC₅₀	16.08 μM Compound: PCI-34051	Antiproliferative activity against human MDA-MB-231 cells by MTT assay Antiproliferative activity against human MDA-MB-231 cells by MTT assay	[PMID: 35661851]
MIA PaCa-2	GI₅₀	>20000 nM Compound: PCI-34051	Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTS assay Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTS assay	[PMID: 30004697]
MIA PaCa-2	IC₅₀	>20000 nM Compound: PCI-34051	Antiproliferative activity against human MIA PaCa-2 cells after 72 hrs by CellTiter Glo assay Antiproliferative activity against human MIA PaCa-2 cells after 72 hrs by CellTiter Glo assay	[PMID: 35797900]
MOLT-4	GI₅₀	3.3 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human MOLT-4 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human MOLT-4 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
MOLT-4	GI₅₀	2.4 μM Compound: 41; PCI-34051	Antiproliferative activity against human MOLT4 cells by alamar blue assay Antiproliferative activity against human MOLT4 cells by alamar blue assay	[PMID: 29505935]
MOLT-4	IC₅₀	9.4 μM Compound: 1; PCI-34051	Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay	[PMID: 29533873]
MT2	GI₅₀	15 μM Compound: 6, PCI-34051	Growth inhibition of human MT2 cells incubated for 72 hrs by MTS assay Growth inhibition of human MT2 cells incubated for 72 hrs by MTS assay	[PMID: 23116147]
MT4	GI₅₀	25 μM Compound: 6, PCI-34051	Growth inhibition of human MT4 cells incubated for 72 hrs by MTS assay Growth inhibition of human MT4 cells incubated for 72 hrs by MTS assay	[PMID: 23116147]
NB1	GI₅₀	14 μM Compound: 6, PCI-34051	Growth inhibition of human NB-1 cells incubated for 72 hrs by MTS assay Growth inhibition of human NB-1 cells incubated for 72 hrs by MTS assay	[PMID: 23116147]
NCI-N87	IC₅₀	1500 nM Compound: PCI-34051	Antiproliferative activity against human NCI-N87 cells after 72 hrs by CellTiter Glo assay Antiproliferative activity against human NCI-N87 cells after 72 hrs by CellTiter Glo assay	[PMID: 35797900]
OVCAR-3	GI₅₀	6 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human OVCAR-3 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human OVCAR-3 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
PBMC	GI₅₀	>100 μM Compound: 6, PCI-34051	Growth inhibition of human PBMC PB-N cells incubated for 72 hrs by MTS assay Growth inhibition of human PBMC PB-N cells incubated for 72 hrs by MTS assay	[PMID: 23116147]
PBMC	GI₅₀	97 μM Compound: 6, PCI-34051	Growth inhibition of human PBMC PB-O cells incubated for 72 hrs by MTS assay Growth inhibition of human PBMC PB-O cells incubated for 72 hrs by MTS assay	[PMID: 23116147]
PC-3	IC₅₀	19.2 μM Compound: 1; PCI-34051	Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay	[PMID: 29533873]
PC-3	GI₅₀	2660 nM Compound: PCI-34051	Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay	[PMID: 30004697]
Raji	GI₅₀	6.8 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human Raji cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human Raji cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
Ramos	GI₅₀	6.1 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human Ramos cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human Ramos cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
RKO	GI₅₀	14 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human RKO cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human RKO cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
RPMI-8226	GI₅₀	28 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human RPMI-8226 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human RPMI-8226 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
SH-SY5Y	IC₅₀	2.38 μM Compound: PCI-34051	Antiproliferative activity against human SH-SY5Y cells by MTT assay Antiproliferative activity against human SH-SY5Y cells by MTT assay	[PMID: 35661851]
SUD4	GI₅₀	8.2 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human SU-DHL-4 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human SU-DHL-4 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
SU-DHL-2	IC₅₀	>5 μM Compound: PCI-34051	Antiproliferative activity against human SU-DHL-2 cells assessed as cell viability measured after 72 hrs by Alamar Blue Assay Antiproliferative activity against human SU-DHL-2 cells assessed as cell viability measured after 72 hrs by Alamar Blue Assay	[PMID: 38949959]
THP-1	GI₅₀	15.4 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human THP-1 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human THP-1 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
THP-1	IC₅₀	>10 μg/mL Compound: PCI-34051	Antileishmanial activity against amastigote stage of Leishmania donovani infected in human THP1 cells after 48 hrs by Alamar blue assay Antileishmanial activity against amastigote stage of Leishmania donovani infected in human THP1 cells after 48 hrs by Alamar blue assay	[PMID: 25240614]
THP-1	IC₅₀	>10 μg/mL Compound: PCI-34051	Cytotoxicity against human THP1 cells after 48 hrs by Alamar blue assay Cytotoxicity against human THP1 cells after 48 hrs by Alamar blue assay	[PMID: 25240614]
THP-1	IC₅₀	>33.3 μM Compound: PCI-34051	Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 39089850]
U-87MG ATCC	GI₅₀	17 μM Compound: Chemical probe: PCI-34051	Anti-proliferative activity against human U87 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay Anti-proliferative activity against human U87 cells assessed as growth inhibition incubated for 72 hrs by alamar blue staining based fluorometric assay	[PMID: 18256683]
U-87MG ATCC	GI₅₀	>15000 nM Compound: PCI-34051	Antiproliferative activity against human U87 cells after 72 hrs by MTS assay Antiproliferative activity against human U87 cells after 72 hrs by MTS assay	[PMID: 30004697]
U-937	EC₅₀	210 μM Compound: PCI-34051	Cytotoxicity against human U937 cells assessed as decrease in cell viability after 44 hrs by MTT assay Cytotoxicity against human U937 cells assessed as decrease in cell viability after 44 hrs by MTT assay	[PMID: 29150330]

In Vitro

PCI-34051 inhibits pure recombinant HDAC8 with K_i of 10 nM with >200-fold selectivity over the other HDACs tested, including HDACs 1, 2, 3, 6 and 10. PCI-34051 is derived from a low molecular weight hydroxamic acid scaffold that possessed promising potency (HDAC8; K_i=2 μM) and selectivity (approximately fivefold) for HDAC8 relative to the other class I HDACs. PCI-34051 is found to induce apoptosis at low micromolar concentrations in cell lines derived from T-cell lymphomas, including Jurkat and HuT78, whereas doses as high as 20 μM has no effect on B-cell- or myeloid-derived lymphomas or solid tumor lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Administration of PCI-34051 and Dexamethasone reduces the eosinophilic inflammation and airway hyperresponsiveness in asthma to reduce the airway remodeling^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 950762-95-5
Appearance Solid
Molecular Weight 296.32
Formel C₁₇H₁₆N₂O₃
Color Off-white to pink
SMILES

COC(C=C1)=CC=C1CN2C3=CC(C(NO)=O)=CC=C3C=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (31)

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Cancer Cell

Fusobacterium nucleatum facilitates anti-PD-1 therapy in microsatellite stable colorectal cancer. [Abstract]

2024 Oct 14;42(10):1729-1746.e8. PMID: 39303724
Cell Metab

Microbial regulation of hexokinase 2 links mitochondrial metabolism and cell death in colitis. [Abstract]

2021 Dec 7;33(12):2355-2366.e8. PMID: 34847376
Cell Host Microbe

Oat-β-glucan potentiates anti-PD-1 efficacy through Faecalibacterium prausnitzii-derived butyrate and indole-3-propionic acid. [Abstract]

2026 Jul 8;34(7):1333-1349.e10. PMID: 42214334
Cancer Res

Targeting the SP/KLF Transcriptional Regulatory Network Synergizes with HDAC Inhibition to Impede Progression of H3K27M Diffuse Intrinsic Pontine Glioma. [Abstract]

2025 Jun 2;85(11):2100-2116. PMID: 40053472
Autophagy

Deacetylation of ATG16L1 is required for LC3-associated lysosomal microautophagy. [Abstract]

2025 Aug 28:1-15. PMID: 40851277
Nucleic Acids Res

HDAC8 cooperates with SMAD3/4 complex to suppress SIRT7 and promote cell survival and migration. [Abstract]

2020 Apr 6;48(6):2912-2923. PMID: 31970414

PCI-34051 purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2020 Apr 6;48(6):2912-2923. [Abstract]

Immunoblotting analysis of SIRT7 level in cells incubated with the HDAC8 inhibitor PCI-34051 (PCI), in the presence or absence of TGF-1 (5 ng/ml).
Theranostics

HDAC1 and 2 regulate endothelial VCAM-1 expression and atherogenesis by suppressing methylation of the GATA6 promoter. [Abstract]

2021 Mar 20;11(11):5605-5619. PMID: 33859766

PCI-34051 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Mar 20;11(11):5605-5619. [Abstract]

HAEC were pretreated with HDAC3 inhibitor RGFP, HDAC8 inhibitor PCI-34051 (PCI; 10, 20 nM) or HDAC1/2 inhibitor Romi, followed by TNF stimulation and Western blot analysis.
Adv Sci (Weinh)

The Probiotic Parabacteroides johnsonii Ameliorates Metabolic Disorders Through Promoting BCAAs to BSCFAs Conversion. [Abstract]

2025 Aug 7:e02624. PMID: 40772426

PCI-34051 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug 7:e02624. [Abstract]

PCI-34051 (1 μM) did not promote the expression of FGF1B in NCM460 cells.
Adv Sci (Weinh)

HDAC6 and USP9X Control Glutamine Metabolism by Stabilizing GS to Promote Glioblastoma Tumorigenesis. [Abstract]

2025 Mar 31:e2501553. PMID: 40162736

PCI-34051 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Mar 31:e2501553. [Abstract]

HDAC inhibitor screening with 10 µm PCI34051 and 2 µm T247, TMP195, and ACY241 in U251 cells. Cells were incubated with the indicated HDAC inhibitors for 24 h.
Cell Death Dis

Global crotonylome reveals hypoxia-mediated lamin A crotonylation regulated by HDAC6 in liver cancer. [Abstract]

2022 Aug 17;13(8):717. PMID: 35977926
Cell Death Dis

Checkpoint regulator B7x is epigenetically regulated by HDAC3 and mediates resistance to HDAC inhibitors by reprogramming the tumor immune environment in colorectal cancer. [Abstract]

2020 Sep 15;11(9):753. PMID: 32934224

PCI-34051 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2020 Sep 15;11(9):753. [Abstract]

The expression of B7x mRNA in Colo-205 cells after treatment with various inhibitors (5 μM) for 48 h (HDAC8 inhibitor: PCI-34051).
Acta Pharmacol Sin

P300/CBP inhibition sensitizes mantle cell lymphoma to PI3Kδ inhibitor idelalisib. [Abstract]

2022 Feb;43(2):457-469. PMID: 33850273
Apoptosis

Valproic acid upregulates the expression of the p75NTR/sortilin receptor complex to induce neuronal apoptosis. [Abstract]

2020 Oct;25(9-10):697-714. PMID: 32712736

PCI-34051 purchased from MedChemExpress. Usage Cited in: Apoptosis. 2020 Oct;25(9-10):697-714. [Abstract]

Effects of HDAC inhibitors on p75NTR and sortilin expression. SH-SY5Y cells were incubated for 24 h with either vehicle, 5 µM tubacin, 30 nM romidepsin, or 5 µM PCI34,051. Cell lysates were analysed for p75NTR and sortilin expression.
EMBO J

Acetylation of TIR domains in the TLR4-Mal-MyD88 complex regulates immune responses in sepsis. [Abstract]

2024 Nov;43(21):4954-4983. PMID: 39294473
Clin Transl Med

Pathogenic variants of TUBB8 cause oocyte spindle defects by disrupting with EB1/CAKP5 interactions and potential treatment targeting microtubule acetylation through HDAC6 inhibition. [Abstract]

2025 Jan;15(1):e70193. PMID: 39834092
Clin Transl Med

A methyltransferase-like 14/miR-99a-5p/tribble 2 positive feedback circuit promotes cancer stem cell persistence and radioresistance via histone deacetylase 2-mediated epigenetic modulation in esophageal squamous cell carcinoma. [Abstract]

2021 Sep;11(9):e545. PMID: 34586732
Cell Rep

Decrypting lysine deacetylase inhibitor action and protein modifications by dose-resolved proteomics. [Abstract]

2024 May 24;43(6):114272. PMID: 38795348
J Med Chem

Discovery of Novel and Highly Potent Dual PD-L1/Histone Deacetylase 6 Inhibitors with Favorable Pharmacokinetics for Cancer Immunotherapy. [Abstract]

2025 Feb 20. PMID: 39979078
J Med Chem

Discovery of a Novel Benzimidazole Derivative Targeting Histone Deacetylase to Induce Ferroptosis and Trigger Immunogenic Cell Death. [Abstract]

2024 Sep 12;67(17):15098-15117. PMID: 39145486
Virulence

The inhibitory and anti-inflammatory effects of TMP269 on peste des petits ruminants virus replication. [Abstract]

2025 Dec;16(1):2495838. PMID: 40275702
J Agric Food Chem

Butyrate Inhibits the HDAC8/NF-κB Pathway to Enhance Slc26a3 Expression and Improve the Intestinal Epithelial Barrier to Relieve Colitis. [Abstract]

2024 Nov 6;72(44):24400-24416. PMID: 39440960
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
iScience

Elevated expression of histone deacetylase HDAC8 suppresses arginine-proline metabolism in necrotizing enterocolitis. [Abstract]

2023 May 14;26(6):106882. PMID: 37260741
Eur J Cell Biol

dCas9-HDAC8-EGFP fusion enables epigenetic editing of breast cancer cells by H3K9 deacetylation. [Abstract]

2024 Oct 18;103(4):151463. PMID: 39437453

PCI-34051 purchased from MedChemExpress. Usage Cited in: Eur J Cell Biol. 2024 Oct 18;103(4):151463. [Abstract]

MCF-7 cells cotransfected with dCas9-HDAC8-EGFP and gRNA-B exhibited statistically significant downregulation of ESR1.Addition of Sulforaphane (2 μM, 24 h) and PCI-34051 (0.5 μM, 24 h) after cotransfection of dCas9-HDAC8-EGFP and gRNA-B in MCF-7 cells resulted in no statistically significant alteration of ESR1 expression.
J Pharmacol Exp Ther

Downregulation of TrkB Expression and Signaling by Valproic Acid and Other Histone Deacetylase Inhibitors. [Abstract]

2019 Sep;370(3):490-503. PMID: 31308194
bioRxiv

2026 Jun 5.
bioRxiv

Butyrate rescues chlorpyrifos-induced social deficits through inhibition of class I histone deacetylases. [Abstract]

2025 Oct 20:2025.10.19.683261. PMID: 41280077
bioRxiv

2023 Jun 5.
Università degli Studi di CAGLIARI

2021 May.
Patent

US20180263995A1.
Methods Mol Biol

Methods for High-throughput Drug Combination Screening and Synergy Scoring. [Abstract]

2018:1711:351-398. PMID: 29344898

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 30 mg/mL (101.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3747 mL

16.8736 mL

33.7473 mL

5 mM

0.6749 mL

3.3747 mL

6.7495 mL

10 mM

0.3375 mL

1.6874 mL

3.3747 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (8.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (8.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

Histone deacetylase activity is measured using a continuous trypsin-coupled assay. For inhibitor characterization, measurements are performed in a reaction volume of 100 μL^-1 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% DMSO, pH 7.4, supplemented with bovine serum albumin at concentrations of 0-0.05% ) is mixed with inhibitor at various concentrations and allowed to incubate for 15 min. Trypsin 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 355 nm and a detection wavelength of 460 nm. The increase in fluorescence with time is used as the measure of the reaction rate. Inhibition constants K_i(app) are obtained using the program BatchK_i^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

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 compound exposure using an Alamar Blue fluorometric cell proliferation assay as recommended by the manufacturer. Compounds (e.g.,PCI-34051) are 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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Mice^[2]
A mouse model of asthma is utilized. Briefly, healthy female BALB/C mice (n=72) aged 6-8 weeks and weighing 18-22 g are used. Animals are housed independently in a pathogen-free room and provided ad libitum access to water and standard food. Animals are housed for 1 week prior to experiment onset. Mice are divided into six treatment groups: normal control, simple asthma, Dexamethasone, Tubastatin A HCl, PCI-34051, and Givinostat. Sensitization is carried out for mice in the last five groups on the 1st, 8th and 15th day using ovalbumin (OVA, 20 μg) and aluminum hydroxide gel (2 mg). 7 days after the last sensitization, OVA (20 mg/mL) atomization is performed using an ultrasonic atomizing device (3 mL/min for 30 min, 3 times/week for 8 weeks). Dexamethasone (2.0 mg/kg), TSA (0.5 mg/kg), PCI-34051 (0.5 mg/kg) and Givinostat (0.5 mg/kg) are administered via intraperitoneal injection 30 min before excitation. In the normal control group, normal saline is used instead of OVA.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Balasubramanian S, et al. A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas. Leukemia. 2008 May;22(5):1026-34. [Content Brief]

[2]. Ren Y, et al. Therapeutic effects of histone deacetylase inhibitors in a murine asthma model. Inflamm Res. 2016 Dec;65(12):995-1008. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.3747 mL	16.8736 mL	33.7473 mL	84.3682 mL
	5 mM	0.6749 mL	3.3747 mL	6.7495 mL	16.8736 mL
	10 mM	0.3375 mL	1.6874 mL	3.3747 mL	8.4368 mL
	15 mM	0.2250 mL	1.1249 mL	2.2498 mL	5.6245 mL
	20 mM	0.1687 mL	0.8437 mL	1.6874 mL	4.2184 mL
	25 mM	0.1350 mL	0.6749 mL	1.3499 mL	3.3747 mL
	30 mM	0.1125 mL	0.5625 mL	1.1249 mL	2.8123 mL
	40 mM	0.0844 mL	0.4218 mL	0.8437 mL	2.1092 mL
	50 mM	0.0675 mL	0.3375 mL	0.6749 mL	1.6874 mL
	60 mM	0.0562 mL	0.2812 mL	0.5625 mL	1.4061 mL
	80 mM	0.0422 mL	0.2109 mL	0.4218 mL	1.0546 mL
	100 mM	0.0337 mL	0.1687 mL	0.3375 mL	0.8437 mL

Keywords

PCI-34051

31 Cited Publications

100 mg Angebot einholen

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PCI-34051

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Osteogenesis Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

RNA Binding Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) PCI-34051

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (31)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PCI-34051 Related Classifications

HY-15224 Related Classifications