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Epigenetics

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Cat. No. Product Name Field of Application Chemical Structure
DC10172 WT-161
WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.
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DC10190 TPOP146
TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
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DC10931 Tianeptinostat
Tianeptinostat is a class I HDAC inhibitor with IC50 of 28, 33 and 51 nM for HDAC1, 2 and 3, respectively, also inhibits HDAC6 (IC50=1.6 nM) but not HDAC5 (IC50>80 uM).
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DC10930 Tianeptinaline
Tianeptinaline is a class I HDAC-selective, brain penetrant analogue of tianeptine with IC50 of 0.24, 0.12 and 0.155 uM for HDAC1, 2 and 3 respectively, does not inhibit HDAC6.
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DC11702 T-3775440
T-3775440 is a novel potent, selecitve, irreversible LSD1 inhibitor with IC50 of 2.1 nM.
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DC11226 T1551
T1551 is a novel selective PRMT5 inhibitor with IC50 of 34.1 uM, decreases cell viability of A549 cell with IC50 of 5.8 uM (72h).
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DC11157 SRTCX1003
SRTCX1003 (SRTCX-1003) is a small molecule activator of SIRT1 (STAC) with EC1.5 of 0.61 uM, enhances deacetylation of cellular p65 protein with IC50 of 1.42 uM in cellular p65 acetylation assay.
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DC11156 SRTCX1002
SRTCX1002 (SRTCX-1002) is a small molecule activator of SIRT1 (STAC) with EC1.5 of 0.4 uM, enhances deacetylation of cellular p65 protein with IC50 of 0.84 uM in cellular p65 acetylation assay.
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DC12109 SIRT5 inhibitor
SIRT5 inhibitor is a potent Human Sirtuin 5 deacylase inhibitor, with an IC50 of 0.11 μM.
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DC8867 SirReal2
SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.
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DC6313 Guadecitabine(SGI-110) Featured
SGI-110 (S-110) is a stable and potent inhibitor for DNA methylation, inhibits DNMT1 when SGI-110 is activated by phosphorylation and incorporated into DNA.
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DC7261 Resminostat hydrochloride (4SC-201)
Resminostat(RAS2410; 4SC-201) is a potent inhibitor of HDAC1/3/6(IC50=43-72 nM); less potent to HDAC8 with IC50 of 877 nM.
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DC11041 QCA276
QCA276 is a novel potent BET proteins inhibitor with IC50/Ki of 10/.3 nM, QCA276 is the BET ligand for PROTAC QCA570.
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DC12248 PROTAC BET degrader-2
PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
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DC11153 PF-06855800
PF-06855800 (PF06855800) is a potent, selective, SAM competitive, BBB-penetrant, orally active inhibitor of protein arginine methyltransferase PRMT5 with Ki of 0.02 nM.
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DC10634 PF-06726304
PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM.
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DC10023 MT-1 Featured
MT1 is a bivalent chemical probe of BET bromodomains.MT1 is an intramolecular bivalent BRD4 binder that is more than 100-fold more potent, in cellular assays, than the corresponding monovalent antagonist, JQ1.
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DC11063 MS645
MS645 (MS-645) is a novel, bivalent bromodomain (BRD) inhibitor with Ki of 18.4 nM for tandem BD1-BD2 (BRD4 BD1/BD2 ), shows12- to 28-fold gain in affinity for binding to the tandem BD1-BD2 over the single BD1 or BD2.
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DC10938 MPT0G211
MPT0G211 is a novel potent, selective HDAC6 inhibitor with IC50 of 0.291 nM, displays >1,000-fold selectivity over other HDAC isoforms.
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DC10951 MPT0E028
MPT0E028 is a potent HDAC inhibitor that inhibits nuclear HDAC activity with IC50 of 11.1 nM in HeLa cells, 9-30 times more potent than SAHA.
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DC11045 miR-21 inhibitor 37
miR-21 inhibitor 37 is a novel inhibitor of miR-21 function with EC50 of 5.3 uM in HeLa-miR21-Luc assays, displays no inhibition of miR-122.
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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).
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DC9934 GNE-272
GNE-272 is a in Vivo Probe for the Bromodomains of CBP/EP300.
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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.
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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.
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DC10413 DDP-38003 dihydrochloride
DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
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DC10968 CPTH6
CPTH6 is a thiazole derivative that can reduce histone acetylation and histone acetyltransferase (HAT) activity in human leukemia cells, CPTH6 is a specific Gcn5/pCAF inhibitor.
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DC10969 CPTH6 hydrobromide
CPTH6 hydrobromide is a thiazole derivative that can reduce histone acetylation and histone acetyltransferase (HAT) activity in human leukemia cells, CPTH6 is a specific Gcn5/pCAF inhibitor.
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DC10970 CPTH2
CPTH2 is a specific histone acetyltransferase inhibitor modulating Gcn5 network in vitro and in vivo, inhibits H3 acetylation and induces cell-cycle perturbation and apoptosis in U-937 cells.
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DC10944 CBB3001
CBB3001 (CBB-3001) is a novel potent, selective histone demethylase LSD1 inhibitor with IC50 of 21.25 uM.
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