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Histone Methyltransferase

Histone methyltransferases are a group of enzymes that catalyze the methylation of histone lysine and arginine by adding methyl groups to specific histone arginine or lysine residues. Histone methyltransferaes can be classified into 3 classes, including SET domain lysine methyltransferases, non-SET domain lysine methyltransferases and arginine methyltransferases (PRMTs), all of which use S-adenosylmethionine as a cosubstrate for the transfer of the methyl group. Aberrant histone methylation has been associated with a wide range of human cancers (such as hematological malignancies), which leads to the development of novel cancer chemotherapies targeting cancer-associated histone methyltransferases (more than 20 lysine methyltransferases and 9 arginine methyltransferases in humans).

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  1. Cat.No. Product Name Information
  2. B1127 UNC 0631 UNC 0631 is a potent inhibitor of Protein lysine methyltransferase G9a (also known as KMT1C or EHMT2) with the IC50 value of 4nM .
  3. B1126 UNC0321 UNC0321 is the most potent small-molecule inhibitor of protein lysine methyltransferase G9a, an enzyme methylating lysine 9 of histone H3 (H3K9) and lysine 373 (K373) of p53, with the inhibition constant Ki value of 63 nM and the half maximal inhibition concentration IC50 values of 9 nM in enzyme-coupled SAH detection assay (ECSD) and 6 nM in chemiluminescence-based oxygen tunneling assay (CLOT) respectively .
  4. B1622 SGI-1027 SGI-1027 is an inhibitor of DNMT with IC50 values of 12.5μM, 8μM and 7.5μM, respectively for DNMT1, DNMT3A and DNMT3B .
  5. A4504 UNC 0646 IC50: 6 nm (G9a IC50); 26 nm (Cellular IC50); 3.3 μM (Cell toxicity EC50)
  6. B1581 EPZ004777 HCl EPZ004777 is a potent and selective inhibitor of DOT1L, a protein methyltransferase catalyzing the methylation of lysine 4 of histone H3 (H3K4), with the half maximal inhibition concentration IC50 value of 400 pM .
  7. A4170 EPZ004777 EPZ004777 is a specific small-molecule H3K79 methyltransferase DOT1L inhibitor that potently inhibits DOT1L in a radionuclide homogeneous assay with the half maximal inhibition concentration IC50 value of 400 pM and selectively kills a variety of MLL-rearranged leukemia cells, including an MLL-AF4 leukemia cell line MV4-11 and an MLL-AF9 leukemia cell line MOLM13 [1 & 2].
  8. A4167 SGC 0946 SGC 0946 is a potent small-molecule inhibitor of protein methyltransferase (PMT) DOT1L, a unique protein lysine methyltransferase (PKMT) catalyzing the methylation of histone H3 on Lysine 79 (H3K79), with the half maximal inhibition concentration IC50 value of 0.3 nM .
  9. B1583 UNC1999 UNC1999 is an orally bioavailable inhibitor of EZH2 and EZH1 with IC50 values of .
  10. B1582 MM-102 MM-102 is an antagonist of MLL1 with IC50 value of 2.4nM .

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