FT895 (FT-895) is a potent and selective inhibitor of HDAC11 with IC50 of 3 nM, displays no significant activity against HDAC1-10 (IC50>5 uM); displays promising cellular activity (IC50<20 nM) and pharmacokinetic properties; FT895 is a useful tool to study the biology of HDAC11 and shows potential use as a therapeutic target for oncology and inflammation indications.
Tubastatin A hydrochloride
Tubastatin A hydrochloride is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in cell-free assays; displays 57-fold selectivity over HDAC8 and >1,000-fold selective against other HDAC isoforms; induces an increase in acetylated-α-tubulin levels and the restoration of primary cilia expression in the cholangiocarcinoma cell lines at 10 uM, shows significant inhibition of TNF-α and IL-6 in LPS stimulated human THP-1 macrophages with IC50 of 272 nM and 712 nM; reduces the growth of cholangiocarcinoma in vivo.
OBP-801 (YM 753;Spiruchostatin A) is a novel cyclic-peptide-based HDAC inhibitor with IC50 of 2 nM; significantly inhibits the cell growth on comparison with each agent alone and synergistically increased apoptosis with the induction of Bim; significantly suppresses tumor growth in vivo.
Phase 1 Clinical
Merck60 (BRD 6929, Compound-60) is a potent, selective and brain-penetrant inhibitor of HDAC1 and HDAC2 with IC50 of 1 nM and 8 nM respectively; displays 50-400 fold selectivity over class I HDAC3 (IC50 = 458 nM) and no appreciable inhibition of HDAC8 or of the class II HDACs (IC50>30 uM); alters gene expression in brain circuits involved in mood regulation, improves mood-related behaviors in mice.
HDAC8-IN-20a is a potent, selective HDAC8 inhibitor with IC50 of 27 nM; efficiently blocks the activation of growth receptor survival signaling and shifts the cell cycle arrest and differentiation phenotype toward effective cell death of neuroblastoma cell lines combined with crizotinib, efficiently kills neuroblastoma cell lines carrying wildtype ALK, amplified ALK and those carrying the activating ALK F1174L mutation, as well as cells carrying the activating R1275Q mutation.
EDO-S101 (Tinostamustine) is a fusion molecule comprising of the alkylator bendamustine and the HDAC-inhibitor vorinostat; displays potent activity in vitro in MM cell lines (IC50=1.6-4.8 uM) and ex vivo in cells isolated from MM patients; shows activity in CB17-SCID murine plasmacytoma model and in de novo Vk*MYC mice, also is the only drug with single-agent activity in the multidrug resistant Vk12653 murine model.
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