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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. B7718 (R)-PFI 2 hydrochloride New Product
  3. A8221 EPZ-6438 EPZ-6438 is a potent and bio-available inhibitor of EZH2, the catalytic subunit of polycomb repressive complex 2 (PRC2) catalyzing the methylation of lysine 27 of histone H3 (H3K27), that inhibits the activity of human PRC2-containing wild-type EZH2 with a value of inhibition constant Ki of 2.5 nM.
  4. A4503 UNC 0224 Potent inhibitor of G9a histone lysine methyltransferase (IC50 = 15 nM).
  5. A1909 BIX 01294 BIX-01294 is a small molecule inhibitor of G9a and GLP (a H3K9 PKMT that shares 80% sequence identity with G9a in their respective SET domains) that was discovered via screening of a library of 125,000 synthetic compounds.
  6. A1908 AMI-1 Potent, cell permeable and specific protein arginine N-methyltransferase 1 (PRMT1) inhibitor (IC50 = 8, 8 µM), Does not compete for the AdoMet (S-adenosyl-L-methionine, SAM) binding site, Blocks peptide substrate binding, HIV-1 RT polymerase inhibitor (IC50 = 5, 0 µM).
  7. A1914 UNC0638 Selective inhibitor of G9a and GLP histone lysine methyltransferases (IC50 values are < 15 nM and 19 nM for G9a and GLP respectively, and > 10000 nM for a range of other histone methyltransferases).
  8. A8182 3-Deazaneplanocin A (DZNep) hydrochloride 3-Deazaneplanocin A (DZNep) hydrochloride is a selective inhibitor of ENZ2 inhibitor with IC50 value of 0.08-0.24 μM.
  9. A4502 Chaetocin Chaetocin, a natural thiodioxopiperazine product from Chaetomium species, is a lysine-specific histone methyltransferase inhibitor, which reduces the histone methyltransferase effects of SUV39H1 with IC50 value of 0.8 μM.
  10. B1256 AZ505 ditrifluoroacetate AZ505 is a potent SET and MYND domain-containing 2 protein (SMYD2) inhibitor that selectively inhibits the enzymatic activity of SMYD2 (IC50: 0.12 μM) over a variety of other protein lysine methyltransferases (IC50 > 83.3 μΜ), including SMYD3, DOT1L, EZH2, GLP, G9A and SET7/9 .
  11. B1255 AZ505 AZ505, a molecule identified from a high throughput chemical screen, is a potent and selective inhibitor of SET and MYND domain-containing 2 protein (SMYD2), a protein lysine methyltransferase catalyzing the methylation of both histone (H2B, H3 and H4) and non-histone protein substrates including the tumor suppressor proteins p53 and Rb, with the half maximal inhibition concentration IC50 and inhibition constant Ki values of 0.12 μM and 0.3 μM respectively.

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