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Epigenetics

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Cat. No. Product Name Field of Application Chemical Structure
DC5183 I-BET151 Featured I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM, respectively.
DC9658 I-BRD9 Featured I-BRD9 is a potent and selective BRD9 inhibitor (pIC50 = 7.3). Exhibits >70-fold selectivity for BRD9 over a panel of 34 other bromodomains and >700-fold selectivity over the BET family.
DC9982 I-CBP112 Featured I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC50 = 0.142 and 0.625 μM, respectively).
DC7487 Pyroxamide Featured Inhibitor of histone deacetylase (HDAC); potently inhibits affinity purified HDAC1. Also inhibits the growth of tumor cells in vitro and in vivo. Induces p21/WAF1 expression in tumor cells.
DC7614 IOX1 Featured IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases.
DC10220 ITSA-1 (ITSA1) Featured ITSA-1 (ITSA1) is an HDAC activator via TSA suppression, but shows no activity towards other HDAC inhibitors.
DC11421 JQEZ5 Featured JQEZ5 is a novel and potent EZH2 inhibitor.
DC10586 KDM4D-IN-1 Featured KDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC50 value of 0.41±0.03 μM.
DC10285 KDM5-IN-1 Featured KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
DC8578 L002(NSC764414) Featured L002 is a p300 inhibitor (IC50=1.98 μM) that inhibits p53 and histone acetylation. Suppresses STAT3 activation in vitro and suppresses tumor growth in some mouse cell lines.
DC7856 LLY-507 Featured LLY-507 is a chemical probe for SMYD2 (a protein lysine methyltransferase).
DC4241 LMK-235 Featured LMK-235 is a selective histone deacetylase (HDAC) 4 and HDAC5 inhibitor (IC50 values are 4.22, 11.9, 55.7, 320, 852, 881, and 1278 nM for HDAC 5, 4, 6, 1, 11, 2, and 8, respectively).
DC8541 ORY-1001(Ladademstat) Featured ORY-1001 dihydrochloride (RG-6016, Ladademstat) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases.
DC11106 Vafidemstat (ORY-2001) Featured Vafidemstat (ORY-2001) is an oral, brain penetrant drug that inhibits LSD1 and MAOB by reducing cognitive impairment, including memory loss and neuroinflammation. It also has neuroprotective effects.
DC10560 MAK683 Featured MAK683 is a novel PRC2/EED inhibitor.
DC5128 MC1568 Featured MC1568 is a class II (IIa) HDAC inhibitor selective for HDAC4 and HDAC6
DC10940 MC3343 Featured MC3343 (MC-3343) is a novel potent, non-nucleoside DNA methyltransferase (DNMT) inhibitor with IC50 of 5.7 and 1.7 uM for DNMT1 and DNMT3a.
DC7794 MG149 Featured MG 149 is an inhibitor of histone acetyltransferases (HAT) with IC50 values of 74μM and 47μM for Tip60 and MOF, respectively.
DC7196 MGCD0103 (Mocetinostat) Featured MGCD0103 (Mocetinostat) is a potent HDAC inhibitor with IC50 of 0.15, 0.29 and 1.66 μM for HDAC 1, HDAC 2 and HDAC 3, respectively.
DC8546 MI-136 Featured MI-136 inhibits DHT-induced expression of androgen receptor (AR) target genes.
DC8544 MI-463 Featured MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
DC8545 MI-503 Featured MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-MLL interaction.
DC10287 MI-538 Featured MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM.
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.
DC9836 Mivebresib(ABBV-075) Featured Mivebresib is a novel BET family inhibitor, disrupts critical transcription programs that drive prostate cancer growth to induce potent anti-tumor activity in vitro and in vivo.
DC7740 ML-324 Featured ML-324 is a JMJD2 histone demethylase inhibitor (JMJD2 IC50 = 920 nM)
DC7562 MM-102 Featured MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.
DC10063 MPI-5a Featured MPI_5a is a potent selective inhibitor of HDAC6, and poorly blocks other HDAC enzymes.
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.
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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