PCI-34051

Catalog No.S2012

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.

1 Customer Review

(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.

Purity & Quality Control

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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	Incubation Time	Activity Description	PMID
human Huh7 cells	M13lPWZ2dmO2aX;uJIF{e2G7	MnXlN{Bl[Xm\|	MUfBcpRqfmm{YXygZYN1cX[rdImgZYdicW6\|dDDIR3Yh\2Wwb4T5dIUhOWJiaX7m[YN1\WRiaX6gbJVu[W5iSIXoO{Bk\WyuczDh[pRmeiB\|IHThfZMh[nlibIXjbYZmemG\|ZTDy[ZBwenSncjDn[Y5mKGG\|c3H5MEBGSzVyPUGuPEDPxE1?	NE\BPVkzPTR7MEewNC=>
human Jurkat cells	NV3iT2VjT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M1TBWFczKGh?	MYDHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDKeZJs[XRiY3XscJMhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgUXRUKGG\|c3H5MEBIUTVyPUGxJO69VQ>?	NVTkWnd{OjNzMU[xOFc>
human NB-1 cells	MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	Mn3NO\|IhcA>?	Mn;iS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUmIuOSClZXzsd{BqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO\|YYmsJGdKPTB;MUSg{txO	MYSyN\|EyPjF2Nx?=
human MT2 cells	MmjOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NXTkWlFwPzJiaB?=	MYjHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNWFIh[2WubIOgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxRTF3IN88US=>	MlXKNlMyOTZzNEe=
human MT4 cells	NGfVZ4dIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MUW3NkBp	M4LqW2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1VPCClZXzsd{BqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO\|YYmsJGdKPTB;MkWg{txO	NX3CboNDOjNzMU[xOFc>

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:^[1]	+ Expand 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]	+ Expand 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)

Kinase Assay:^[1]

+ Expand

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]

+ Expand

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): 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 Download PCI-34051 SDF

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

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PCI-34051