PCI-34051HDAC8 inhibitor,potent and selective CAS# 950762-95-5 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 950762-95-5 | SDF | Download SDF |
| PubChem ID | 24753719 | Appearance | Powder |
| Formula | C17H16N2O3 | M.Wt | 296.32 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 30 mg/mL (101.24 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | N-hydroxy-1-[(4-methoxyphenyl)methyl]indole-6-carboxamide | ||
| SMILES | COC1=CC=C(C=C1)CN2C=CC3=C2C=C(C=C3)C(=O)NO | ||
| Standard InChIKey | AJRGHIGYPXNABY-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C17H16N2O3/c1-22-15-6-2-12(3-7-15)11-19-9-8-13-4-5-14(10-16(13)19)17(20)18-21/h2-10,21H,11H2,1H3,(H,18,20) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent and selective histone deacetylase 8 (HDAC8) inhibitor (IC50 = 10 nM). Displays >200 fold selectivity over HDAC isoforms 1, 2, 3, 6 and 10. Induces apoptosis in cell lines derived from T cell lymphomas or leukemias. |
PCI-34051 Dilution Calculator
PCI-34051 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.3747 mL | 16.8737 mL | 33.7473 mL | 67.4946 mL | 84.3683 mL |
| 5 mM | 0.6749 mL | 3.3747 mL | 6.7495 mL | 13.4989 mL | 16.8737 mL |
| 10 mM | 0.3375 mL | 1.6874 mL | 3.3747 mL | 6.7495 mL | 8.4368 mL |
| 50 mM | 0.0675 mL | 0.3375 mL | 0.6749 mL | 1.3499 mL | 1.6874 mL |
| 100 mM | 0.0337 mL | 0.1687 mL | 0.3375 mL | 0.6749 mL | 0.8437 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
Reference
S Balasubramanian, J Ramos, W Luo, M Sirisawad, E Verner, J J Buggy. A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas. Leukemia (2008) 22, 1026–1034.
Sriram Balasubramanian, Erik Verner, Joseph J. Buggy. Isoform-speci?c histone deacetylase inhibitors: The next step? Cancer Letters. Volume 280, Issue 2, 8 August 2009, Pages 211–221.
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A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas.[Pubmed:18256683]
Leukemia. 2008 May;22(5):1026-34.
We have developed a potent, histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 with >200-fold selectivity over the other HDAC isoforms. PCI-34051 induces caspase-dependent apoptosis in cell lines derived from T-cell lymphomas or leukemias, but not in other hematopoietic or solid tumor lines. Unlike broad-spectrum HDAC inhibitors, PCI-34051 does not cause detectable histone or tubulin acetylation. Cells defective in T-cell receptor signaling were still sensitive to PCI-34051-induced apoptosis, whereas a phospholipase C-gamma1 (PLCgamma1)-defective line was resistant. Jurkat cells showed a dose-dependent decrease in PCI-34051-induced apoptosis upon treatment with a PLC inhibitor U73122, but not with an inactive analog. We found that rapid intracellular calcium mobilization from endoplasmic reticulum (ER) and later cytochrome c release from mitochondria are essential for the apoptotic mechanism. The rapid Ca(2+) flux was dependent on PCI-34051 concentration, and was blocked by the PLC inhibitor U73122. Further, apoptosis was blocked by Ca(2+) chelators (BAPTA) and enhanced by Ca(2+) effectors (thapsigargin), supporting this model. These studies show that HDAC8-selective inhibitors have a unique mechanism of action involving PLCgamma1 activation and calcium-induced apoptosis, and could offer benefits including a greater therapeutic index for treating T-cell malignancies.
Histone deacetylase inhibitor treatment dramatically reduces cholesterol accumulation in Niemann-Pick type C1 mutant human fibroblasts.[Pubmed:21436030]
Proc Natl Acad Sci U S A. 2011 Apr 5;108(14):5620-5.
Niemann-Pick type C (NPC) disease is predominantly caused by mutations in the NPC1 protein that affect intracellular cholesterol trafficking and cause accumulation of unesterified cholesterol and other lipids in lysosomal storage organelles. We report the use of a series of small molecule histone deacetylase (HDAC) inhibitors in tissue culture models of NPC human fibroblasts. Some HDAC inhibitors lead to a dramatic correction in the NPC phenotype in cells with either one or two copies of the NPC1(I1061T) mutation, and for several of the inhibitors, correction is associated with increased expression of NPC1 protein. Increased NPC1(I1061T) protein levels may partially account for the correction of the phenotype, because this mutant can promote cholesterol efflux if it is delivered to late endosomes and lysosomes. The HDAC inhibitor treatment is ineffective in an NPC2 mutant human fibroblast line. Analysis of the isoform selectivity of the compounds used implicates HDAC1 and/or HDAC2 as likely targets for the observed correction, although other HDACs may also play a role. LBH589 (panobinostat) is an orally available HDAC inhibitor that crosses the blood-brain barrier and is currently in phase III clinical trials for several types of cancer. It restores cholesterol homeostasis in cultured NPC1 mutant fibroblasts to almost normal levels within 72 h when used at 40 nM. The findings that HDAC inhibitors can correct cholesterol storage defects in human NPC1 mutant cells provide the potential basis for treatment options for NPC disease.
