| 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. |
| M11019 | UNC6934 | UNC6934 is a chemical probe that targets the PWWP domain of NSD2 and locates kernels. |
| M10845 | LEM-14 | |
| M10532 | Tazemetostat hydrobromide | Tazemetostat (EPZ-6438) hydrobromide is a first-in-class potent, selective and orally available EZH2 inhibitor. |
| M9449 | PFI-2 hydrochloride | PFI-2 hydrochloride is a potent, highly selective and cell-active inhibitor of the methyltransferase activity of SETD7, with IC50 of 2 nM. |
| M9442 | CM-272 | CM-272 is a first-in-class, reversible dual small molecule inhibitor of G9a and DNMTs in hematologic malignancies. |
| M9151 | MI-503 | MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM. |
| M9150 | MI-463 | MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the Menin-MLL interaction, with an IC50 value of 15.3 nM. |
| M9145 | MI-2 | MI-2 (Menin-MLL Inhibitor 2) is a potent menin-MLL interaction inhibitor with IC50 of 446±28 nM. |
| M9004 | WDR5-0103 | WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 µM). |
| M8989 | BIX-01294 | BIX-01294 is a potent chemical inhibitor of G9a methyltransferase that catalyzes the mono-and di-methylation of the lysine 9 residue of histone H3, with IC50 of 1.9 μM. |
| M8933 | EPZ011989 | EPZ011989 is a potent, orally-available EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646. |
| M8529 | A-366 | A-366 is a potent and highly selective peptide-competitive inhibitor of histone methyltransferase G9a, with IC50s of 3.3 nM and 38 nM for G9a and GLP, respectively, and is more than 1,000-fold selective for G9a and GLP over 21 other methyltransferases. A-366 is also a potent inhibitor of Spindlin1-H3K4me3 interaction (IC50=182.6 nM).A-366 shows high affinity for human H3R (Ki=17 nM) and exhibits subtype selectivity between subpopulations of the histaminergic and dopaminergic receptor families. It can be used for induction and maintenance of pluripotent stem cells in mice. |
| M8475 | OICR-9429 | OICR-9429 is a cell penetrant, potent and selective antagonist of the interaction of WDR5 (WD repeat domain 5) with peptide regions of MLL and Histone 3 that potently binds to WDR5. |
| M8397 | BRD4770 | BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 inhibited the dimethylation and trimethylation of H3K9, EC50 was 5 µM, and had little effect on H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 activates the ataxic telangiectasia mutation (ATM) pathway and induces cell senescence. |
| M8196 | Sinefungin | Sinefungin blocks the methylation of bases in DNA and RNA, such as 5-methylcytosine or N6-methyladenosine, suggesting a role in gene expression. |
| M7578 | SGC0946 | SGC0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM; selectively kill mixed lineage leukaemia cells. |
| M7509 | UNC0642 | UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels. |
| M7508 | JQ-EZ-05 | JQ-EZ-05 is a specific and reversible EZH1/2 inhibitor. |
| M7458 | UNC3866 | UNC3866 is a high affinity CBX4 and CBX7 inhibitor. UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen (IC50=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel. |
| M6592 | Chaetocin | Chaetocin is a specific inhibitor of the histone methyltransferase (HMT) SU(VAR)3-9 with an IC50 of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase (TrxR) with an IC50 of 4 μM. |
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