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Histone Methyltransferase Histone methyltransferase

Cat.No.  Name Information
M2358 3-Deazaneplanocin A 3-deazaneplanocin A (DZNeP), an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM.
M21488 CM-579 CM-579 is a first-in-class reversible dual inhibitor of G9a and DNA methyltransferase (DNMT) with IC50 values of 16 nM and 32 nM, respectively. It plays an active role in a variety of cancer cells.
M21306 UNC6852 UNC6852 is a PROTAC technology-based, selective PRC2 degradation agent containing an EED ligand and a von Hippel-Lindau ligand with an IC50 value of 247 nM for EED action.
M21119 CPI-1328 CPI-1328 is an EZH2 inhibitor with a Ki value of 63 fM.
M20623 LLY-284 LLY-284 is the diastereomer of LLY-283, which is a potent and selective SAM-competitive chemical probe for PRMT5. LLY-284 is much less active than LLY-283 and can be used as a negative control for LLY-283.
M20492 AMI-1, free acid AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.
M13850 SGC3027 SGC3027 is a histone methyltransferase inhibitor. SGC3027 is the first potent, selective and cell active chemical probe for PRMT7.
M13846 EPZ011989 trifluoroacetate EPZ011989 trifluoroacetate is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.
M13843 BRD9539 BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1.
M13840 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.
M11278 GNA002 GNA002 is a potent, selective, covalent EZH2 inhibitor with an IC50 of 1.1 μM against EZH2. GNA002 can specifically and covalently bind Cys668 in the EZH2-SET domain to induce EZH2 degradation through COOH terminal of ubiquitination mediated by Hsp70 interacting protein (CHIP). GNA002 effectively reduced EZH2-mediated H3K27 trimethylation and reactivated tumor suppressor genes silenced by Polycomb repressor complex 2 (PRC2).
M11169 DM-01 DM-01 is a potent and selective EZH2 inhibitor that can be used to study diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 gene-related solid tumors.
M11019 UNC6934 UNC6934 is a chemical probe that targets the PWWP domain of NSD2 and locates kernels.
M10860 MRK-740 MRK-740 is a potent, selective, substrate-competitive PRDM9 histone methyltransferase inhibitor,IC50 80 nM. MRK-740 is more selective to PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 Reduces PRDM9-Dependent H3K4 Trimethylation (IC50 0.8 μM).
M10796 BI-9321 BI-9321 is a potent, selective, cell-active NSD3-PWWP1 antagonist,Kd The value is 166 nM. BI-9321 is not valid for NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts NSD3-PWWP1 interaction with histones in U2OS cells,IC50 1.2 μM.




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