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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| 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). |
| M9003 | MS023 | MS023 is a potent and selective, cell-active inhibitor of type I PRMTs with IC50s of 4-119 nM. |
| 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. |
| 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. |
| M6312 | LLY-283 | LLY-283 is the potent and selective SAM-competitive chemical probe for PRMT5. It inhibits PRMT5 enzyme activity with IC50 of 20 nM for methylation of an H4R3 derived peptide substrate, and shows greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. |
| M6288 | LLY-507 | LLY-507 is a cell-active, potent, and selective inhibitor of protein-lysine Methyltransferase SMYD2. |
| M6177 | SGC2085 | SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs. |
| M6142 | XY1 | XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), but XY1 is completely inactive. |
| M5412 | Amodiaquin dihydrochloride dihydrate | Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase in human erythrocytes, also used as an antimalarial and anti-inflammatory agent. |
| M5186 | CPI-360 | CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM. |
| M5163 | SGC707 | SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively. |
| M5128 | PFI-2 | PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets. |
| 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. |
| M2334 | EPZ004777 | EPZ004777 is a potent, selective, small-molecule inhibitor of DOT1L with IC50 of 0.4 nM. |
| M2179 | EPZ-5676 | EPZ-5676 is a potent and selective aminonucleoside inhibitor of DOT1L histone methyltransferase. |
| M2024 | BIX 01294 Trihydrochloride | BIX 01294 Trihydrochloride is a potent inhitor of G9a histone methyltransferase with IC50 of 2.7 μM. |
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