950762-95-5 Usage
Uses
Used in Oncology:
PCI 34051 is used as a targeted therapy for T-cell lymphomas and leukemias due to its ability to induce caspase-dependent apoptosis in cell lines derived from these cancers. Its specificity for HDAC8 makes it a promising candidate for the treatment of these malignancies.
Used in Niemann-Pick Type C1 Disease:
PCI 34051 is used as a potential treatment for Niemann-Pick type C1 disease, a rare genetic disorder characterized by the accumulation of cholesterol and other lipids in cells. Its ability to significantly reduce cholesterol accumulation in Niemann-Pick type C1 gene mutated human fibroblasts suggests its potential therapeutic value in managing this condition.
Used in Drug Development:
PCI 34051 serves as a valuable tool in drug development, particularly in the discovery and optimization of HDAC inhibitors. Its specificity for HDAC8 allows researchers to study the role of this enzyme in various diseases and develop targeted therapies with minimal side effects.
Biological Activity
pci-34051 is a potent, specific inhibitor of histone deacetylase 8 (hdac8) with greater than 200-fold selectivity over the other hdac isoforms, such as 1, 2, 3, 6 and 10. it induces caspase dependent apoptosis in cell lines derived from t-cell lymphomas or leukemias, but not in other hematopoietic or solid tumor lines. pci-34051 does not cause detectable histone or tubulin acetylation and also does not inhibit growth or induce apoptosis in normal cells such as pbmcs or fibroblasts. although a phospholipase c-gamma1 (plcgamma1) defective line is resistant, cells defective in t-cell receptor signaling are still sensitive to pci-34051 induced apoptosis.
Check Digit Verification of cas no
The CAS Registry Mumber 950762-95-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,5,0,7,6 and 2 respectively; the second part has 2 digits, 9 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 950762-95:
(8*9)+(7*5)+(6*0)+(5*7)+(4*6)+(3*2)+(2*9)+(1*5)=195
195 % 10 = 5
So 950762-95-5 is a valid CAS Registry Number.
950762-95-5Relevant academic research and scientific papers
INDOLE DERIVATIVES AS INHIBITORS OF HISTONE DEACETYLASE
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, (2008/06/13)
Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the acitivy of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
