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PCI-34051HDAC8 inhibitor,potent and selective

PCI-34051

Catalog No. A4091
Size Price Stock Qty
Evaluation Sample $28.00 In stock
10mg $110.00 In stock
100mg $710.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

PCI-34051

Biological Activity

Description PCI-34051 is a potent and specific inhibitor of HDAC8 with an IC50 value of 10 nM.
Targets HDAC8 HDAC6 HDAC1 HDAC10 HDAC2 HDAC3
IC50 10 nM 2.9 μM 4 μM 13 μM >50 μM >50 μM

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Chemical Properties

Cas No. 950762-95-5 SDF Download SDF
Synonyms PCI34051, PCI 34051
Chemical Name N-hydroxy-1-[(4-methoxyphenyl)methyl]indole-6-carboxamide
Canonical SMILES COC1=CC=C(C=C1)CN2C=CC3=C2C=C(C=C3)C(=O)NO
Formula C17H16N2O3 M.Wt 296.32
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
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.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

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.