hyperacetylation

PTACH (Cpd 51) (NCH-51) is a SAHA-based inhibitor of human HDAC. It can potently inhibit the growth of various human Y cells (EC50: 1 to 10 μM).

Trichostatin A (TSA), a natural derivative of diene isohydroxamic acids, is a specific and reversible histone deacetylase inhibitor (IC50=1.8 nM) that induces hyperacetylation of core histones to regulate chromatin structure.

Triciferol acts as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR ( IC 50 =87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Triciferol also exhibits efficacious antiproliferative and cytotoxic activities in cancer cell models in vitro [1].

HDAC-IN-82 (Compound 18b) is a histone deacetylase (HDAC) inhibitor that demonstrates selective antimalarial and anticancer activities. It shows significant antiproliferative and caspase3 7 activity in tumor cells. Additionally, HDAC-IN-82 induces hyperacetylation of histone H3 and α-tubulin.

Cambinol (SIRT1 2 Inhibitor IV) is a cell-permeable b-naphthol compound that inhibits the NAD-dependent deacetylase activity of SIRT1 2 (IC50: 56 59 μM, respectively) in a substrate-, but not NAD-, competitive manner. Cambinol inhibits SIRT5 deacetylase activity only at much higher concentrations (IC50 >300 μM) and no inhibitory for the class I and II HDACs. In BCL6-expressing Burkitt lymphoma cell lines, Cambinol-induced apoptosis has been attributed to the hyperacetylation of p53 and BCL6.Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)

Sirt1 2-IN-1 (Compound 7) is an inhibitor of SIRT1 and SIRT2, with IC50 values of 1.81 μg mL for SIRT1, 2.10 μg mL for SIRT2, and 20.5 μg mL for SIRT3, and exhibits α-microtubulin hyperacetylation activity, demonstrating significant anticancer effects.

MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) when compared with LNCaP (IC50, 0.97 μM) and PC3 cells (IC50, 5.12 μM). MHY219 showed a potent inhibition of total HDAC activity when compared with SAHA. MHY219 increased histone H3 hyperacetylation and reduced the expression of class I HDACs (1, 2 and 3) in prostate cancer cells. MHY219 effectively increased the sub-G1 fraction of cells through p21 and p27 dependent pathways in DU145 cells. MHY219 significantly induced a G2 M phase arrest in DU145 and PC3 cells and arrested the cell cycle at G0 G1 phase in LNCaP cells. Furthermore, MHY219 effectively increased apoptosis in DU145 and LNCaP cells, but not PC3 cells, according to Annexin V PI staining and Western blot analysis. These results indicate that MHY219 is a potent HDAC inhibitor that targets regulating mu......

HDAC6 degrader-3, a selective and potent degrader of HDAC6 through ternary complex formation and the ubiquitin-proteasome pathway, exhibits a DC50 value of 19.4 nM. With IC50 values of 4.54 nM for HDAC6 and 0.647 μM for HDAC1, it effectively induces robust hyperacetylation of α-tubulin [1].

Compound A5b, also known as JMJD3 HDAC-IN-1, is a dual inhibitor that targets both JMJD3 (Jumonji domain-containing protein demethylase 3) and HADC1 (histone deacetylase, IC50 = 16 nM). It induces hypermethylation of histone H3K27 and hyperacetylation of H3K9, while also promoting apoptosis through the cleavage of caspase-7 and PARP. This compound has demonstrated the ability to effectively inhibit cancer cell cloning, migration, and invasion [1].

Valproic Acid-d15 is a deuterated compound of Valproic Acid. Valproic Acid has a CAS number of 99-66-1. Valproic Acid is a branched chain fatty acid which potentially enhances central GABAergic neurotransmission and inhibits Na+ channels. Currently, the various molecular mechanisms of action of Valproic Acid have not been completely elucidated. Valproic Acid has been reported to be a potent inhibitor of histone deacetylases (HDACs) in vitro. Valproic Acid is also noted to relieve HDAC-dependent transcriptional repression and causes the hyperacetylation of histones in cultured cells. Additionally, Valproic Acid is reported to activate Wnt-dependent gene expression and to mimic trichostatin A (sc-3511) in the inhibition of histone deacetylase.

Valproic Acid-d4 is a deuterated compound of Valproic Acid. Valproic Acid has a CAS number of 99-66-1. Valproic Acid is a branched chain fatty acid which potentially enhances central GABAergic neurotransmission and inhibits Na+ channels. Currently, the various molecular mechanisms of action of Valproic Acid have not been completely elucidated. Valproic Acid has been reported to be a potent inhibitor of histone deacetylases (HDACs) in vitro. Valproic Acid is also noted to relieve HDAC-dependent transcriptional repression and causes the hyperacetylation of histones in cultured cells. Additionally, Valproic Acid is reported to activate Wnt-dependent gene expression and to mimic trichostatin A (sc-3511) in the inhibition of histone deacetylase.

2-(Propyl-3,3,3-d3)pentanoic-5,5,5-d3 Acid is a deuterated compound of 2-pentanoic Acid. 2-pentanoic Acid has a CAS number of 99-66-1. Valproic Acid is a branched chain fatty acid which potentially enhances central GABAergic neurotransmission and inhibits Na+ channels. Currently, the various molecular mechanisms of action of Valproic Acid have not been completely elucidated. Valproic Acid has been reported to be a potent inhibitor of histone deacetylases (HDACs) in vitro. Valproic Acid is also noted to relieve HDAC-dependent transcriptional repression and causes the hyperacetylation of histones in cultured cells. Additionally, Valproic Acid is reported to activate Wnt-dependent gene expression and to mimic trichostatin A (sc-3511) in the inhibition of histone deacetylase.