Toll Free: (877) 796-6397 -- USA and Canada only -- |
Fax: +1-832-582-8590 Orders: +1-832-582-8158 |
Tech Support: +1-832-582-8158 Ext:3 Please provide your Order Number in the email. |
Formula | C17H16N2O3 |
||||||
Molecular Weight | 296.32 | CAS No. | 950762-95-5 | ||||
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) |
|
||||||
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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. PCI-34051 induces caspase-dependent apoptosis. | ||
---|---|---|---|
Targets |
|
||
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] |
||
In vivo | PCI-34051 is a potent and specific HDAC8 inhibitor. |
Kinase Assay: |
|
---|---|
Cell Assay: |
|
Animal Study: |
|
|
Data from [Data independently produced by , , Exp Mol Med, 2017, 49(2):e297]
Data from [Data independently produced by , , Stem Cells Transl Med, 2018, doi:10.1002/sctm.18-0057]
Inhibition of HDAC8 mitigates AKI by reducing DNA damage and promoting homologous recombination repair [ J Cell Mol Med, 2024, 28(18):e70114] | PubMed: 39317961 |
Establishing a Drug Screening Platform for Polycystic Kidney Disease in Kidney Organoids [ The University of Auckland, 2023, ] | PubMed: none |
Corroborating evidence for aberrant expression of histone deacetylase 8 in endometriosis [ Reprod Med Biol, 2023, 22(1):e12527] | PubMed: 37476367 |
Corroborating evidence for aberrant expression of histone deacetylase 8 in endometriosis [ Reprod Med Biol, 2023, 10.1002/rmb2.12527] | PubMed: 37476367 |
Aberrant expression of histone deacetylase 8 in endometriosis and its potential as a therapeutic target [ Reprod Med Biol, 2023, 22(1):e12531] | PubMed: 37564680 |
Histone deacetylase 8 regulates NF-κB-related inflammation in asthmatic mice through H3K9 acetylation [ Chin Med J (Engl), 2022, 135(17):2110-2112.] | PubMed: 35170504 |
TOB1 attenuates IRF3-directed antiviral responses by recruiting HDAC8 to specifically suppress IFN-β expression [ Commun Biol, 2022, 5(1):943] | PubMed: 36085336 |
Repression of the PRELP gene is relieved by histone deacetylase inhibitors through acetylation of histone H2B lysine 5 in bladder cancer [ Clin Epigenetics, 2022, 14(1):147] | PubMed: 36371227 |
HDAC2 Is Involved in the Regulation of BRN3A in Melanocytes and Melanoma [ Int J Mol Sci, 2022, 23(2)849] | PubMed: 35055045 |
Development of Human Adrenocortical Adenoma (HAA1) Cell Line from Zona Reticularis [ Int J Mol Sci, 2022, 24(1)584] | PubMed: 36614027 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.