epigenetics

LLY-507 is an effective, cell-active, and specific inhibitor of protein-lysine Methyltransferase SMYD2.

LP99 is an epigenetic probe. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells. LP99 is an effective and selective inhibitor of the BRD7 and BRD9 bromodomains (Kd: 99 nM against BRD9).

Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycetes, functioning as an XBP1 inhibitor and inhibiting IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM), and induces apoptosis.

A-366 is a highly selective peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP, respectively.It is more than 1,000-fold selective for G9a and GLP over the other 21 methyltransferases. It is an inhibitor of the Spindlin1-H3K4me3 interaction with an IC50 of 182.6 nM.It exhibits high affinity for human H3R with a Ki value of 17 nM, and shows subtype selectivity between subgroups of the histaminergic and dopaminergic receptor families.

Bobcat339 is a novel cytosine-based TET enzyme inhibitor (IC50s: 33 73 uM for TET1 2), but not DNMT3a, does not inhibit the DNA methyltransferase DNMT3a.

GSK-5959 is an effective, specific and cell permeable BRPF1 bromodomain inhibitor (IC50: ~80 nM). The selectivity of GSK-5959 for BRPF1 is >100-fold over a panel of 35 other bromodomains, including BRPF2 3 and BET family bromodomains.

BAY-474 is an inhibitor of tyrosine-protein kinase c-Met. It acts as an epigenetics probe

CM-272 is a dual G9a DNA methyltransferases (DNMTs) inhibitor.

Larsucosterol trimethylamine (DUR-928 trimethylamine) is a potent liver X receptor (LXR) antagonist that modulates endogenous epigenetics, reduces lipid accumulation in hepatocytes, attenuates lipopolysaccharide (LPS) and TNFα-induced inflammatory responses in macrophages, and alleviates LPS- and acetaminophen (ATMP)-induced multi-organ damage.

KAT modulator-1 (Compound 3), an epigenetics research tool, selectively interacts with the full-length p300 protein but not its catalytic domain [1].