Histone Deacetylation

Apicidin (183506-66-3) is a fungal toxin that is a potent, cell permeable inhibitor of histone deacetylases (HDAC's).1 It also displays antitumor properties by inducing changes in p21WAF1/Cip1 and gelsolin gene expression...

BML-278 is a structurally novel activator of SIRT1 (EC50=1 μM). Displays selectivity over SIRT2 and 3 (EC50=25 and 50 μM respectively). Cell permeable. References/Citations1) Mai et al. (2009), Study of...

A novel hybrid dual-acting HDAC and receptor tyrosine kinase inhibitor. It is a potent HDAC inhibitor which also inhibits EGFR and HER2,  IC50 = 4.4, 2.4 and 15.7 nM respectively.1 It not only blocks EGFR and HER2 but...

HPA (96017-59-3) is a histone deacetylase (HDAC) inhibitor, IC50=13 μM1. More potent and robust than valproic acid at inducing histone hyperacetylation (600% at 50 μM), HSP70 induction and protection against glutamate...

MS-275 (Entinostat - 209783-80-2) is a potent HDAC inhibitor. Selective for HDAC1 (IC50 = 300 nM) over HDAC3 (IC50 = 8 μM) and HDAC8 (IC50 100 μM).1 In vivo, MS-275, has been shown to inhibit tumor growth via induction...

Panobinostat (404950-80-7) is a potent inhibitor of class I and II HDACs.1 Cotreatment with panobinostat and an HSP90 inhibitor caused synergistic apoptosis in human CML-BC and AML cells.2 A potent antimyeloma...

Piceatannol (10083-24-6) is a naturally occurring analog of resveratrol (Cat.# 10-1057). Inhibits nonreceptor kinases Syk and Lyk (IC50 approximately 10 μM)1. Piceatannol stimulates Sirt12. References/Citations1) Seow et...

Romidepsin (128517-07-7) is a potent and selective inhibitor of class I histone deacetylases (HDACs), IC50 = 36, 47, 510 and 14,000 nM for HDAC1, 2, 4 and HDAC6, respectively.1 Induces apoptosis in a variety of cell...

SirtAct (839699-72-8) is a Sirt1 activator (233% at 10 μM)1 Suppresses TNFα release from THP-1 cells and stimulates adipogenesis in 3T3L1 cells1. SIRT1 stimulation by SirtAct leads to decreased tissue factor...

Splitomycin (5690-03-9) was initially shown to inhibit Sir2p (the yeast Sirt1 homolog) and create a conditional phenocopy of a sir2 deletion mutant in S. cerevisiae1. Cells grown in the presence of the drug have silencing...