Table 3.

HDACi (Partial List)

ClassCompoundStructureHDAC Target (Potency)Effects on Transformed CellsStage of Development (Reference)
HydroxamatesTSAEmbedded ImageClass I and II (nmol/L)TD; GA; A; AI; AEN/C
SAHA, Zolinza, vorinostatEmbedded ImageClass I and II (μmol/L)TD; GA; AI; AE; MF; AU; S; PP; ROS-CDMerck Food and Drug Administration approved for CTCL (4)
CBHAEmbedded ImageN/A (μmol/L)GA; A; AI; AEMerck (4)
LAQ-824Embedded ImageClass I and II (nmol/L)GA; A; AINovartis phase I (discontinued)
PDX-101Embedded ImageClass I and II (μmol/L)GA; ATopoTarget phase II (57)
LBH-589Embedded ImageClass I and II (nmol/L)GA; A; ROS-CDNovartis phase I (51)
ITF2357Embedded ImageClass I and II (nmol/L)GA; A; AIItalfarmaco phase I (56)
PCI-24781NAClass I and II (NA)N/APharmacyclics phase I
Cyclic peptideDepsipeptide (FK-228)Embedded ImageClass I (nmol/L)TD; GA; A; AI; AE; MF; ROS-CDGloucester Pharmaceuticals phase IIb for CTCL and PTCL (63) phases I and II
Aliphatic AcidsValproic AcidEmbedded ImageClass I and IIa (mmol/L)TD; GA; A; SAbbot phase II
Phenyl butyrateEmbedded ImageClass I and IIa (mmol/L)TD; GA; A; AI; AEPhase II
ButyrateEmbedded ImageClass I and IIa (mmol/L)TD; GA; A; AI; AEPhase II
AN-9Embedded ImageN/A (μmol/L)TD; GA; ATitan Pharmaceuticals phase II
BenzamidesMS-275Embedded ImageHDAC1, HDAC2, HDAC3 (μmol/L)TD; GA; A; AI; AE; ROS-CDSchering AG phase II (51)
MGCD0103Embedded ImageClass I (μmol/L)TD; GA; AMethylgene phase II (60)
  • Abbreviations: GA, growth arrest; TD, terminal differentiation; A, apoptosis; AI, cell death by activating intrinsic apoptotic pathway; AE, cell death by activating extrinsic apoptotic pathway; MF, mitotic failure; AU, autophagic cell death; S, senescence; PP, polyploidy; ROS-CD, reactive oxygen species–facilitated cell death; N/A, not available; CBHA, M-carboxycinnamic acid bishydroxamate; CTCL, cutaneous T-cell lymphoma; CTCL, peripheral T-cell lymphoma.