PCI-34051 950762-95-5

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Molecular Weight:

296.32 PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM. It has greater than 200-fold selectivity over HDAC1 and 6, more than 1000-fold selectivity over HDAC2, 3, and 10.






Biological Activity


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.

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Product Categories : Epigenetics > HDAC Inhibitor