Inhibitors

Active Motif's Zebularine is a DNA methyltransferase inhibitor which binds covalently to methyltransferases. Zebularine re-activates silenced E-cad...

Active Motif's UNC1999 is an orally active, highly selective inhibitor of both wild-type and mutant EZH1 and EZH2 lysine methyltransferases (IC50 =...

Active Motif's The DNA damage response protein 53BP1 utilizes its tandem tudor domain to recognize dimethylated lysine 20 on histone (H4K20me2), a ...

Active Motif's Potent and selective histone deacetylase 6 (HDAC 6) inhibitor (IC50 = 15 nm; >1000-fold selective against other HDACs and 60-fold...

Active Motif's Triacetyl resveratrol is a resveratrol prodrug. One method for increasing the half-life of resveratrol in vivo is acetylation of the...

Active Motif's TC-E-5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor (IC50 = 1.5 uM). It displays no activity against CAR...

Active Motif's Splitomicin is a Sirtuin inhibitor that was initially shown to inhibit Sir2p (the yeast Sirt1 homolog) and create a conditional phen...

Active Motif's SirtAct is a sirtuin activator (Sirt1). It suppressed TNF-alpha release from THP-1 cells and stimulated adipogenesis in 3T3L1 cells....

Active Motif's Sinefungin is a Nucleoside S-adenosyl-1-methionine analog. It is a potent, competitive methyltransferase (protein, DNA, and RNA meth...

Active Motif's SGC707 is a potent and selective allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3), IC50 = 31 nM and selective ag...

Active Motif's Salermide is a SIRT1 and SIRT2 inhibitor. It exhibits a stronger inhibitory effect on SIRT2 than on SIRT1 in vitro. Salermide induce...

Active Motif's RVX-208 is a potent BET bromodomain antagonist with (IC50 = 0.51 uM for BD2) with approximately 170-fold selectivity over BD1 (ref 1...

Active Motif's RG108 is a non-nucleoside DNA methyltransferase inhibitor (IC50 = 115 nM). It inhibits DNA methylation in human and tumor cell lines...

The JARID1 (Jumonji AT-Rich Interactive Domain 1) family of lysine demethylases is responsible for demethylation of trimethylated lysine 4 in histo...

Active Motif's NSC-663284 is a potent and selective inhibitor of the protein lysine methyltransferase SETD8 (IC50 = 0.21 uM) which efficiently supp...

Active Motif's Mocetinostat is a Class I, isoform-selective HDAC inhibitor (IC50 = 0.15, 0.29, 1.66 and 0.59 uM for HDAC1, 2, 3 and 11 respectively...

Active Motif's ML-324 inhibits JMJD2 histone demethylases (JMJD2 IC50 = 920 nM). It represses the expression of viral (HCMV and HSV-1) immediate ea...

Active Motif's Mithramycin A inhibits DNA methyltransferase. A selective Sp1 inhibitor, it binds to GC-rich DNA sequences, displacing Sp1 transcrip...

Active Motif's JIB-04 is a novel specific inhibitor of the Jumonji family of histone demethylases in vitro, in cancer cells and in tumors in vivo. ...

Active Motif's GSK-J4 is an inhibitor of the histone demethylase JMJD3/UTX. It inhibits demethylation of histone H3K27. GSK-J4 reduces LPS-induced ...

Active Motif's Embelin inhibits the lysine acetyltransferase PCAF in vitro and in vivo (in vitro IC50 = 7.2 uM). It inhibits H3K9 acetylation in mo...