Epigenetics

Epigenetics is the control of gene expression without altering the DNA sequence, including DNA methylation, genomic imprinting, maternal effects, gene silencing, nucleolus dominant, dormant transposon activation, and RNA editing. In contrast to classical genetics, which focuses on the effects of gene sequences on biological functions, epigenetics focuses on the mechanisms by which these "epigenetic phenomena" are established and maintained.

Cat. No.	Product name
BP13897	GSK778
BP13897	GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis.
BP13896	GSK778 hydrochloride
BP13896	GSK778 hydrochloride hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 hydrochloride hydrochloride phenocopies the effects of pan-BET inhibitors in cancer models.
BP13895	GSK6853
BP13895	GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain.
BP13894	GSK620
BP13894	GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics.GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood.
BP13893	GSK-5959
BP13893	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.
BP13892	GSK591
BP13892	GSK591, Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).
BP13891	GSK503
BP13891	GSK-503, a potent EZH2 inhibitor, has potential antitumor activity.
BP13890	GSK484 hydrochloride
BP13890	GSK484 hydrochloride (GTPL8577) is a specifc and reversible peptidyl arginine deiminase 4 (PAD4) inhibitor. It demonstrates high-affinity binding to PAD4 with IC50s of 50 nM in the absence of Calcium.
BP13889	GSK467
BP13889	GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).
BP13888	GSK3685032
BP13888	GSK3685032 is a non-covalent and selective DNMT1 inhibitor(IC50 = 36 nM). The inhibitory effect is time-independent and reversible. GSK3685032 induces loss of DNA methylation and transcriptional activation and inhibits cancer cell growth.
BP13887	GSK-3484862
BP13887	Gsk-3484862 is a non covalent inhibitor of DNA methyltransferase DNMT1 with anticancer activity. Gsk-3484862 mediates the global demethylation of mouse embryonic stem cells.
BP13886	GSK3368715 3HCl
BP13886	GSK3368715, a potent inhibitor of type I protein arginine methyltransferases (PRMT), could inhibit PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM.
BP13885	GSK3368715
BP13885	GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.
BP13884	GSK3368715 dihydrochloride
BP13884	GSK3368715 dihydrochloride is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.
BP13883	GSK3326595
BP13883	GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).
BP13882	GSK2879552 2HCl (1401966-69-5(free base))
BP13882	GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
BP13881	GSK2879552
BP13881	GSK2879552 is a selective, orally bioavailable, irreversible, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor, with potential antineoplastic activity.
BP13880	GSK2807 Trifluoroacetate
BP13880	GSK2807 Trifluoroacetate is a selective and SAM-competitive inhibitor of SMYD3 (Ki: 14 nM; IC50: 130 nM).
BP13879	GSK199
BP13879	GSK199 is a selective PAD4 inhibitor(IC50 of 200 nM in the absence of calcium).
BP13878	GSK1379725A
BP13878	GSK1379725A is a selective BPTF ligand (Kd = 2.8 μM).