Lysine Methyltransferases

Lysine methyltransferases are enyzmes that catalyze the transfer of methyl groups from S-adenosylmethionine (SAM) to the lysine residues on histones, particularly histones H3 and H4. The dysregulation of this methylation is critical in the development of cancer.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
6167 A 196
Potent and selective SUV420H1/H2 inhibitor
5163 A 366
Potent and selective G9a/GLP inhibitor
3364 BIX 01294
GLP and G9a inhibitor
6282 BRD 4770
G9a inhibitor and S-adenosyl methionine mimetic; cell permeable
4504 Chaetocin
SUV39H1 inhibitor
0996 Cyproheptadine hydrochloride
SETD7/9 inhibitor; also 5HT2 antagonist
4703 3-Deazaneplanocin A hydrochloride
EZH2 histone methyltransferase inhibitor
5567 EPZ 004777
Highly potent DOT1L inhibitor
6128 GSK 343
Potent and selective SAM-competitive EZH2 inhibitor
5365 LLY 507
Potent SMYD2 inhibitor
6169 PF 06726304 acetate
Highly potent and SAM-competitive EZH2 inhibitor
4892 (R)-PFI 2 hydrochloride
Potent and selective SETD7 inhibitor
5400 (S)-PFI 2 hydrochloride
Negative control of (R)-PFI 2 hydrochloride (Cat. No. 4892)
2609 Ryuvidine
SETD8 inhibitor; also CDK4 inhibitor
4541 SGC 0946
Highly potent and selective DOT1L inhibitor; cell permeable
3861 UNC 0224
Potent G9a and GLP inhibitor
4343 UNC 0638
Selective G9a and GLP inhibitor
5132 UNC 0642
Potent and selective G9a and GLP inhibitor
4342 UNC 0646
Potent and selective G9a and GLP inhibitor
4904 UNC 1999
Potent and selective EZH2/EZH1 inhibitor
4930 UNC 2399
Biotinylated UNC 1999 (Cat.No. 4904)
4905 UNC 2400
Negative control of UNC 1999 (Cat. No. 4904)

Other

Cat No Product Name / Activity
4707 MI 2 dihydrochloride
Menin-MLL interaction inhibitor
5307 MM 102
WDR5/MLL interaction inhibitor
5267 OICR 9429
High affinity and selective WDR5 antagonist
5323 WDR5 0103
WDR5 antagonist

Lysine methyltransferases, or KMTs, are enzymes that catalyze the transfer of methyl groups from S-adenosylmethionine (SAM) to the lysine residues on histones. Upward of 24 human protein lysine methyltransferases have been described and they belong to the histone methyltransferase group of enzymes, which also includes protein arginine methyltransferases. They are also closely related in biological activity to the DNA methyltransferases.

Histones represent the major protein component of chromatin, around which DNA is coiled within the nucleus. Modification of histone protein by methylation induces chromatin remodeling which in turn alters gene expression. Histone methylation is an integral epigenetic process during development and represents an important mechanism of transcriptional regulation and chromatin remodeling. Dysregulation of histone methylation has been implicated in diseases including cancer.

Histone methylation by KMTs occurs predominantly on lysine residues in histones H3 and H4, and multiple methyl groups may be added to each residue.The epigenetic effects of histone methylation are dependent on the residue undergoing methylation and the degree of methylation. Consequently different types of lysine methylation are associated with different functions in the regulation of gene expression. Lysine methylation can induce both transcriptional activation and silencing.

External sources of pharmacological information for Lysine Methyltransferases :

    Literature for Lysine Methyltransferases

    Cancer

    Cancer Research Product Guide

    A collection of over 750 products for cancer research, the guide includes research tools for the study of:

    • Cancer Metabolism
    • Epigenetics in Cancer
    • Receptor Signaling
    • Cell Cycle and DNA Damage Repair
    • Angiogenesis
    • Invasion and Metastasis
    Epigenetics

    Epigenetics Scientific Review

    Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

    Lysine Methyltransferase Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    Euchromatic histone-lysine N-methyltransferase 1 (GLP) Human EHMT1 NM_024757 Q9H9B1
    Mouse Ehmt1 NM_001012518 Q5DW34
    Rat Ehmt1 NM_001108572 NP_001102042
    Euchromatic histone-lysine N-methyltransferase 2 (G9a) Human EHMT2 NM_006709 Q96KQ7
    Mouse Ehmt2 NM_145830 Q9Z148
    Rat Ehmt2 NM_212463 NP_997628
    SET domain containing 2 Human SETD2 NM_014159 Q9BYW2
    Mouse Setd2 NM_001081340 E9Q5F9
    Rat Setd2 NM_001108189 NP_001101659
    SET domain containing (lysine methyltransferase) 7 (SET9) Human SETD7 NM_030648 Q8WTS6
    Mouse Setd7 NM_080793 Q8VHL1
    Rat Setd7 NM_001109558 NP_001103028
    SET domain containing (lysine methyltransferase) 8 Human SETD8 NM_020382 Q9NQR1
    Mouse Setd8 NM_001310723 Q2YDW7
    Rat Setd8 NM_001246665 NP_001233594
    SET domain, bifurcated 1 Human SETDB1 NM_001145415 Q15047
    Mouse Setdb1 NM_001163641 O88974
    Rat Setdb1 XM_002726023 NP_001258104
    SET domain, bifurcated 2 Human SETDB2 NM_031915 Q96T68
    Mouse Setdb2 NM_001081024 Q8C267
    Rat Setdb2 XM_224248 XP_224248
    SET domain containing 1A Human SETD1A NM_014712 O15047
    Mouse Setd1a NM_178029 Q80V17
    Rat - - -
    SET domain containing 1B Human SETD1B XM_037523 Q9UPS6
    Mouse Setd1b NM_001040398 Q8CFT2
    Rat Setd1b XM_219358 XP_219358
    Nuclear receptor binding SET protein domain 1 Human NSD1 NM_172349 Q96L73
    Mouse Nsd1 NM_008739 O88491
    Rat Nsd1 NM_00107337 NP_001100807
    SET and MYND domain containing 2 Human SMYD2 NM_020197 Q9NRG4
    Mouse Smyd2 NM_026796 Q8R5A0
    Rat Smyd2 NM_206851 Q7M6Z3
    PR domain containing 2m with ZNF domain Human PRDM2 NM_012231 Q13029
    Mouse Prdm2 NM_001081355 A2A7B5
    Rat Prdm2 NM_001077648 Q63755