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.
Corin is a dual action LSD1/HDAC inhibitor (IC50=0.33/0.20 uM) that potently targets the CoREST complex and shows more sustained inhibition of CoREST complex HDAC activity compared with entinostat; exhibits a superior anti-proliferative profile against several melanoma lines and cutaneous squamous cell carcinoma lines compared to its parent monofunctional inhibitors but is less toxic to melanocytes and keratinocytes; demonstrates effectivity in slowing tumor growth in a melanoma mouse xenograft model.
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.
ACY-775 (ACY775) is a potent and specific HDAC6 inhibitor (IC50=7.5 nM) with improved brain bioavailability; 60-1500 fold selectivity over class I HDACs; no activity against all other class II HDAC isoforms (IC50>1 uM); induce dramatic increases in α-tubulin acetylation in brain and stimulate mouse exploratory behaviors; increases the innervation of the neuromuscular junctions in the gastrocnemius muscle and improves the motor and sensory nerve conduction in the mutant HSPB1-induced CMT2 mouse model.
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.
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