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Epigenetics

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Cat. No. Product Name Field of Application Chemical Structure
DC47122 KDM2B-IN-4
KDM2B-IN-4 is a histone demethylase KDM2B inhibitor extracted from patent WO2016112284A1, compound 182b. KDM2B-IN-4 can be used for the research of cancer.
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DC46276 BRD0639 Featured
BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities.
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DC46692 NRD167
NRD167 is a potent and selective SIRT5 inhibitor.
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DC46563 UNC4976
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
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DC46460 EZH2-IN-4
EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity.
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DC46442 EHMT2-IN-1
EHMT2-IN-1 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disorder or cancer.
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DC46432 L-Moses dihydrochloride
L-Moses (L-45) dihydrochloride is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM.
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DC46400 INCB059872
INCB059872 is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 can be used for the research of myeloid leukemia.
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DC46389 I-BET151 dihydrochloride
I-BET151 dihydrochloride (GSK1210151A dihydrochloride) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.
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DC46375 MS31
MS31 is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 potently inhibits binding of trimethyllysine-containing peptides to SPIN1. MS31 is not toxic to nontumorigenic cells.
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DC46364 EEDi-5285
EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity.
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DC46286 FTX-6058
FTX-6058 is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). FTX-6058 can induce HbF protein expression in cell and murine models. FTX-6058 can be used for the research of select hemoglobinopathies, including sickle cell disease and β-thalassemia.
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DC46285 FTX-6058 hydrochloride
FTX-6058 hydrochloride is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). FTX-6058 hydrochloride can induce HbF protein expression in cell and murine models. FTX-6058 hydrochloride can be used for the research of select hemoglobinopathies, including sickle cell disease and β-thalassemia.
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DC46269 SW2_110A
SW2_110A is a selective chromobox 8 chromodomain (CBX8 ChD) inhibitor with a Kd of 800 nM. SW2_110A shows minimal 5-fold selectivity for CBX8 ChD over all other CBX paralogs in vitro.
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DC46262 ZEN-3411
ZEN-3411 is a BET inhibitor with IC50s of 0.05, 0.05 and 0.06 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3411 can be used to form PROTACs to induce degradation of BRD4.
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DC46045 KA2507 hydrochloride
KA2507 hydrochloride is a potent and highly selective inhibitor of HDAC6 (IC50=2.5 nM) with no significant toxicities. KA2507 hydrochloride shows antitumor efficacy and immune modulatory effects.
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DC46042 GSK040
GSK040 is a potent and highly selective BET BD2 inhibitor, with a pIC50 of 8.3. GSK040 shows more than 5000-fold selectivity for BET BD2 over BET BD1 (pIC50=4.6). GSK040 can be used for the research of oncology and immunology diseases.
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DC45905 DDO-2093
DDO-2093 is a potent MLL1-WDR5 protein-protein interaction inhibitor (IC50=8.6 nM; Kd=11.6 nM) with antitumor activity. DDO-2093 selectively inhibits the catalytic activity of MLL complex.
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DC45859 EZH2-IN-5
EZH2-IN-5 is a potent EZH2 inhibitor with IC50 values of 1.52 nM and 4.07 nM for wild-type and mutant Tyr641 EZH2, respectively.
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DC45850 CSV0C018875
CSV0C018875 is a quinoline-based EHMT2/G9a inhibitor. CSV0C018875 exhibits lesser cytotoxicity than BIX-01294.
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DC45796 M-1211
M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.
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DC45561 NiCur
NiCur is a potent and selective CBP HAT inhibitor with an IC50 value of 0.35 μΜ. NiCur can be used for performing mechanistic studies without affecting the expression of target proteins.
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DC45560 DCH36_06
DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity.
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DC45559 5-Aza-4'-thio-2'-deoxycytidine
5-Aza-4'-thio-2'-deoxycytidine (5-Aza-T-dCyd) is an orally active DNA methyltransferase I (DNMT1) inhibitor. 5-Aza-4'-thio-2'-deoxycytidine, a sulfur-containing deoxy-cytidine analog, has the potential for DNA hypomethylating and has antitumor effects.
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DC45388 Pomiferin
Pomiferin (NSC 5113) acts as an potential inhibitor of HDAC, with an IC50 of 1.05 μM, and also potently inhibits mTOR (IC50, 6.2 µM).
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DC45335 3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol
3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol, a SIRT1 activator, exhibits significant stimulation of SIRT1 activity. Anti-tumor activity.
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DC45272 7-Chloro-4-(piperazin-1-yl)quinoline
7-Chloro-4-(piperazin-1-yl)quinolone is an important scaffold in medicinal chemistry. 7-Chloro-4-(piperazin-1-yl)quinolone is a potent sirtuin inhibitor and also inhibits the serotonin uptake (IC50 of 50 μM). 7-Chloro-4-(piperazin-1-yl)quinolone exhibits antimalarial activity on D10 and K1 strains of P. falciparum with IC50s of 1.18 μM and 0.97 μM, respectively.
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DC45271 SRT3657
SRT3657 is a brain-permeable activator of SIRT1, with neuroprotective effect.
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DC45270 CHIC35
CHIC35, an analog of EX-527, is a potent and selective inhibitor of SIRT1 (IC50=0.124 µM). CHIC35 shows potential selective inhibition against SIRT1 over SIRT2 (IC50=2.8 µM) or SIRT3 (IC50>100 µM). CHIC35 has anti-inflammatory effects and can be used for CHARGE syndrome research.
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DC44921 AZ506
AZ506 is a potent SMYD2 inhibitor with an IC50 of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal.
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