PCI-34051
For research use only. Not for use in humans.
Catalog No.S2012
17 publications
Molecular Weight(MW): 296.32
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.
2 Customer Reviews
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(d) Effects of HDAC8 activity on ISO-induced augmentation of apoptosis and TIPRL expression. H1299 cells were sequentially treated with 10 μm PCI-34051 for 24 h, ISO for 30 min and 50 μM cisplatin for 48 h before the western blot analysis.
Exp Mol Med, 2017, 49(2):e297. PCI-34051 purchased from Selleck.
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(A): Real‐time PCR to detect TP53 mRNA expression in FD BMSCs treated with PCI‐34051 (15 μM) for 48 hours. (B): Western blot analysis of HDAC8, TP53, and H3K9Ac in FD BMSCs treated with PCI‐34051 for 48 hours compared with the control. (C): Cell proliferation was assessed in a BrdU assay. Scale bar, 100 μm. (D): Apoptotic analysis of FD BMSCs treated with HDAC8 inhibitor for 12 hours. (E): FD BMSCs treated with PCI‐34051 for 48 hours exhibited higher expression of cleaved PARP and cleaved Caspase3 than that in the control. The levels of osteogenesis markers of two group cells induced for 7 days were analyzed by (F) real‐time PCR and (G) Western blot.
Stem Cells Transl Med, 2018, doi:10.1002/sctm.18-0057. PCI-34051 purchased from Selleck.
Purity & Quality Control
Choose Selective HDAC Inhibitors
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. | ||||||||||||||||||||||||||||||||||||||||||||
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| In vitro |
PCI-34051 possesses promising potency for HDAC8 with a Ki of 10 nM. PCI-34051 has high selectivity (approximately fivefold) for HDAC8 relative to the other class I HDACs including HDAC1. PCI-34051 reveals greater than 200-fold selectivity over HDAC1 and HDAC6, and greater than 1000-fold selectivity over HDAC2, HDAC3 and HDAC10. PCI-34051 inhibits ovarian tumor line OVCAR-3 with a GI50 of 6 μM and 15% cell death. Neither significant tubulin nor histone acetylation is observed in the sensitive cell lines treated with PCI-34051 at concentrations less than 25 μM at 24 hours nor at earlier timepoints. PCI-34051 induces a selective cytotoxic effect in cell lines derived only from T-cell malignancies. PCI-34051 induces caspase-dependent apoptosis. When caspase-3 activity is measured at various times after treatment with 5 μM PCI-34051, increasing levels of activity are observed from 12 to 24 to 48 hours, another hallmark of apoptosis, consistent with the higher levels of caspase activity at this timepoint. PCI-34051 does not stimulate Bid cleavage, a characteristic effect of the extrinsic apoptotic pathway. While P116 and J.RT3-T.5 are sensitive to PCI-34051, the PLCγ1-deficient J.gamma1 line reveals a marked decrease in the extent of PCI-34051-induced apoptosis. In addition, steady-state calcium levels strongly influence the apoptosis induced by PCI-34051. PCI-34051 induces cytochrome c release from mitochondria.[1] |
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| Assay |
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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. |
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| Cell Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 59 mg/mL (199.1 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% PEG400+0.5% Tween80+5% propylene glycol For best results, use promptly after mixing. |
30 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 |
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| Formula | C17H16N2O3 |
| CAS No. | 950762-95-5 |
| Storage | powder |
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| Synonyms | N/A |
| Smiles | COC1=CC=C(C[N]2C=CC3=C2C=C(C=C3)C(=O)NO)C=C1 |
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