| 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. |
| M29200 | OTS186935 trihydrochloride | OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells. |
| M29199 | OTS186935 | OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells. |
| M29185 | 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. |
| M28991 | EPZ028862 | EPZ028862 is a selective SMYD3 inhibitor for cancer research. |
| M28971 | A-893 | A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC50 of 2.8 nM. |
| M28933 | ZLD1039 | ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis. |
| M28726 | GSK3368715 | GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity. |
| M28443 | MM-401 | MM-401 is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 µM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia. |
| M28427 | UNC2400 | UNC2400 is a close analog of UNC1999 with >1,000-fold lower potency than UNC1999 as a negative control for cell-based studies. |
| M27953 | MR837 | MR837 is an inhibitor of NSD2-PWWP1. MR837 can bind with human nuclear receptor binding SET domain protein 2 (PWWP domain). |
| M27917 | MS0124 | MS0124 is a potent selective G9a-like protein (GLP) inhibitor with IC50 values of 13±4 nM and 440±63 nM for GLP and G9a,respectively. |
| M27667 | CMP-5 hydrochloride | CMP-5 hydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 hydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 hydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected. |
| M27612 | PR5-LL-CM01 | PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies. |
| M25326 | SMYD3-IN-2 | SMYD3-IN-2 is a SMYD3 inhibitor against gastric cancer via inducing lethal autophagy. SMYD3-IN-2 has inhibitory for SMYD3 and BGC823 cells with IC50 values of 0.81 μM and 0.75 μM, respectively. SMYD3-IN-2 can be used for the research of cancer. |
| M21507 | AS-99 TFA | AS-99 TFA is the first-in-class, effective and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemia activity. In vivo, AS-99 TFA blocked cell proliferation, induced apoptosis and apoptosis, down-regulated MLL fusion target genes, and alleviated leukaemia. |
| M21505 | AS-99 | AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with antileukemic activity. |
| M21504 | AS-99 free base | AS-99 is the first-in-class, effective and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemia activity. |
| 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. |
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