| Identification | Back Directory | [Name]
PCI 34051 | [CAS]
950762-95-5 | [Synonyms]
PCI 34051
PCI-34051
1-(4-methoxybenzyl)-N-hydroxy-1H-indole-6-carboxamide
N-hydroxy-1-(4-Methoxybenzyl)-1H-indole-6-carboxaMide
N-Hydroxy-1-[(4-methoxyphenyl)methyl]-1H-indole-6-carboxamide
1H-Indole-6-carboxamide, N-hydroxy-1-[(4-methoxyphenyl)methyl]- | [Molecular Formula]
C17H16N2O3 | [MDL Number]
MFCD11114393 | [MOL File]
950762-95-5.mol | [Molecular Weight]
296.321 |
| Chemical Properties | Back Directory | [density ]
1.25 | [storage temp. ]
2-8°C | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥14.8 mg/mL in DMSO | [form ]
Powder | [pka]
9.16±0.30(Predicted) | [color ]
White to gray | [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) | [InChIKey]
AJRGHIGYPXNABY-UHFFFAOYSA-N | [SMILES]
N1(CC2=CC=C(OC)C=C2)C2=C(C=CC(C(NO)=O)=C2)C=C1 |
| Hazard Information | Back Directory | [Usage]
PCI-34051 is a potent, histone deacetylase 8 (HDAC8)-specific inhibitor. PCI-34051 induces caspase-dependent apoptosis in cell lines derived from T-cell lymphomas or leukemias. PCI-34051 did not affect other hematopoietic or solid tumor lines. PCI-34051 treatment has been shown to significantly reduce cholesterol accumulation in Niemann-Pick type C1 gene mutated human fibroblast. | [Uses]
PCI-34051 is a potent, histone deacetylase 8 (HDAC8)-specific inhibitor. PCI-34051 induces caspase-dependent apoptosis in cell lines derived from T-cell lymphomas or leukemias. PCI-34051 did not affect other hematopoietic or solid tumor lines. PCI-34051 treatment has been shown to significantly reduce cholesterol accumulation in Niemann-Pick type C1 gene mutated human fibroblast. | [Definition]
ChEBI: N-hydroxy-1-[(4-methoxyphenyl)methyl]-6-indolecarboxamide is an indolecarboxamide. | [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. | [in vivo]
Administration of PCI-34051 and Dexamethasone reduces the eosinophilic inflammation and airway hyperresponsiveness in asthma to reduce the airway remodeling[2]. | [IC 50]
HDAC8: 10 nM (IC50); HDAC6: 2.9 μM (IC50); HDAC1: 4 μM (IC50); HDAC10: 13 μM (IC50) | [storage]
-20°C | [References]
[1]. 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.
[2]. sriram balasubramanian, erik verner, joseph j. buggy. isoform-specific histone deacetylase inhibitors: the next step? cancer letters. volume 280, issue 2, 8 august 2009, pages 211–221. |
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| Company Name: |
J & K SCIENTIFIC LTD.
|
| Telephone: |
18210857532 18210857532 |
| Website: |
https://www.jkchemical.com |
| Company Name: |
NCE Biomedical Co.,Ltd.
|
| Telephone: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
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| Website: |
www.spiropharma.com.cn |
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