PCI 34051 Chemical Properties

Density 

1.25

storage temp. 

Sealed in dry,Store in freezer, under -20°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

Safety Information

Hazard Codes 

Xn

Risk Statements 

22-36

Safety Statements 

26

PCI 34051 Usage And Synthesis

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

IC 50

HDAC8: 10 nM (IC₅₀); HDAC6: 2.9 μM (IC₅₀); HDAC1: 4 μM (IC₅₀); HDAC10: 13 μM (IC₅₀)

storage

-20°C

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