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Epigenetics

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Cat. No. Product Name Field of Application Chemical Structure
DC6909 Entinostat (MS-275) Featured Entinostat (MS-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, compared with HDACs 4, 6, 8, and 10. Phase 1/2.
DC7927 EPZ011989 Featured EPZ011989 is a potent, orally-available EZH2 Inhibitor.
DC8012 EPZ015666 Featured EPZ015666 is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
DC9267 EPZ015866 Featured EPZ015866(GSK591) is a potent, selective PRMT5 inhibitor.
DC9822 EPZ020411 HCl Featured EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has >10 fold selectivity for PRMT6 over PRMT1 and PRMT8.
DC10887 EPZ031686 Featured EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively.
DC4242 Pinometostat(EPZ5676) Featured EPZ-5676 is a small molecule inhibitor of histone methyltransferase with potential antineoplastic activity.
DC10679 EZM2302 Featured EZM2302 (GSK3359088) is the first potent and selective inhibitor of CARM1 enzymatic activity that exhibits anti-proliferative effects both in vitro and in vivo,in biochemical assays (IC50=6nM) with broad selectivity against histone methyltransferases.
DC10845 FL-411 Featured FL-411 is a selective BRD4 inhibitor.
DC11235 Furamidine dihydrochloride Featured Furamidine dihydrochloride (NSC 305831) tyrosyl-DNA phosphodiesterase (Tdp1), also is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with IC50 of 9.4 uM.
DC11071 Gambogenic acid Gambogenic acid (GNA) is a polyprenylated xanthone isolated from gamboge, shows potent antitumor activity and can effectively inhibit the survival and proliferation of cancer cells.
DC7432 Givinostat (ITF2357) Featured Givinostat (ITF2357) is a potent HDAC inhibitor for maize HD2, HD1B and HD1A with IC50 of 10 nM, 7.5 nM and 16 nM. Phase 1/2.
DC11070 GNA002 GNA002 (GNA-002) is a gambogenic acid (GNA) derivative that specifically and covalently binds to Cys668 within the EZH2-SET domain, trigges EZH2 degradation (IC50=1.1 uM) through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination.
DC9934 GNE-272 GNE-272 is a in Vivo Probe for the Bromodomains of CBP/EP300.
DC12313 GNE-371 GNE-371 is a potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like, with an IC50 of 10 nM for TAF1(2).
DC11729 GNE-781 Featured GNE-781 is a potent, selective, non-CNS penetrant, orally active CBP/p300 bromodomain inhibitor with IC50 of 0.94/1.2 nM in TR-FRET assays.
DC5147 Molibresib (I-BET-762) Featured GSK 525762A is a potent small molecule inhibitors that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4).
DC8360 GSK 5959 Featured GSK 5959 is a potent, cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM).
DC8766 GSK1324726A (I-BET726) Featured GSK1324726A (I-BET726) is a novel, potent, and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50= 41 nM), BRD3 (IC50= 31 nM), and BRD4 (IC50= 22 nM).
DC10886 GSK2807 Featured GSK-2807 (GSK 2807, GSK2807) is a potent and selective, SAM-competitive inhibitor of SMYD3 with Ki of 14 nM.
DC8491 GSK2879552 Featured GSK2879552 is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
DC9715 CHR5154 Featured GSK3117391 (CHR5154) is a HDAC inhibitor.
DC10647 EPZ015938(pemrametostat) Featured GSK3326595(EPZ015938) is the first-in-class protein arginine methyltransferase-5 (PRMT5) inhibitor.
DC7143 GSK-343 Featured GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.
DC8044 GSK503 Featured GSK503 is a specific EZH2 methyltransferase inhibitor.
DC9831 GSK6853 Featured GSK6853 is a potent, soluble, cell active, and highly selective inhibitor of the BRPF1 bromodomain
DC8828 HDAC inhibitor IV Featured HDAC inhibitor IV is a cell-permeable pimeloylanilide compound that acts as a FXN- (frataxin gene) specific HDAC (histone deacetylase) inhibitor.
DC11594 HDAC8-IN-20a HDAC8-IN-20a is a potent, selective HDAC8 inhibitor with IC50 of 27 nM.
DC9678 HLCL-61 hydrochloride Featured HLCL-61 is a first-in-class small-molecule inhibitor of PRMT5 for treatment of acute myeloid leukemia.
DC7962 HPOB Featured HPOB is a novel selective inhibitor of HDAC6 catalytic activity in vivo and in vitro.

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