Histone Methyltransferase
Histone modifications play critical roles in regulating both global and stage-specific gene expression. Methylation on histones H3K4, H3K36 and H3K79 is generally associated with gene activation, whereas methylation on histones H3K9 and H3K27 is generally associated with gene repression. Histone lysine methylation is dynamically regulated by site-specific methyltransferases and demethylases. EZH2 (the catalytic subunit of PRC2) is responsible for the methylation of H3K27 in cells.
DOT1L is a histone H3 lysine 79 methyltransferase whose inhibition increases the yield of induced pluripotent stem cells (iPSCs). EPZ-5676 is a potent and selective DOT1L inhibitor.
Crucial to PRC2 activity, the histone methyltransferase enhancer of zeste homolog 2 (EZH2) tri-methylates lysine 27 of histone 3 (H3K27me3), leading to chromatin condensation and transcriptional repression.
Histone Methyltransferase Isoform Specific Products
-
Histone Methyltransferase
(368)
View all products
-
EZH1
(11)
View all products
-
EZH2
(85)
View all products
-
DOT1L
(21)
View all products
-
SMYD2
(9)
View all products
-
SMYD3
(9)
View all products
-
SUV39H2/
KMT1B (4)View all products
-
EHMT2/
G9a/ (32)KMT1C View all products
-
EHMT1/
GLP/ (20)KMT1D View all products
-
ASH1L/
KMT2H (4)View all products
-
SETDB1/
KMT2G (4)View all products
-
SETD2/
KMT3A (5)View all products
-
NSD2/
MMSET/ (16)WHSC1 View all products
-
NSD3/
WHSC1L1 (4)View all products
-
SETD7/
KMT7 (6)View all products
-
SETD8/
KMT5A (5)View all products
-
PRMT1
(25)
View all products
-
PRMT3
(17)
View all products
-
PRMT4
(19)
View all products
-
PRMT5
(64)
View all products
-
PRMT6
(23)
View all products
-
PRMT7
(8)
View all products
-
PRMT8
(13)
View all products
All Product Categories
-
Histone Methyltransferase Inhibitors
(517)
View all products
-
Histone Methyltransferase Agonists
(5)
View all products
-
Histone Methyltransferase Antagonists
(11)
View all products
-
Histone Methyltransferase Activators
(5)
View all products
-
Histone Methyltransferase Modulators
(4)
View all products
-
Histone Methyltransferase Chemical
(1)
View all products
-
Histone Methyltransferase Inducers
(3)
View all products
-
Histone Methyltransferase Degraders
(68)
View all products
-
Histone Methyltransferase Controls
(8)
View all products
-
Histone Methyltransferase Ligands
(16)
View all products
-
Histone Methyltransferase Related Products (687)
Related Products (687)
-
Antibodies (84)
-
Histone Methyltransferase Isoform Comparison
-
UNC7096
0 ImagesCat. No.: HY-155817UNC7096 (compound 53) is a biotinylated affinity reagent. The phenyl ring of UNC7096 replaces the pyrimidine ring in UNC6934 (HY-145103) and introduces biotin at the para position of the phenyl ring, which has a high binding affinity to the NSD2-PWWP1 domain (Kd=46 nM). UNC7096 blocks the interaction between NSD2-PWWP1 and nucleosomal H3K36me2 by occupying the methyl-lysine binding pocket of NSD2-PWWP1. This binding is achieved by covalent binding through the formation of hydrogen bonds and a specific aromatic cage structure. UNC7096 can be used to capture proteins that interact with the NSD2-PWWP1 domain to further analyze the biological significance of these interactions.
-
PROTAC EZH2 Degrader-45
0 ImagesCat. No.: HY-181414CAS No.: 3093642-26-0PROTAC EZH2 Degrader-45 (compound 61) is a PROTAC protein degrader targeting EZH2 with an IC50 of 22.97 μM in SU-DHL-6 cells. PROTAC EZH2 Degrader-45 can be used for the research of diffuse large b-cell lymphoma.
-
EPZ004777 formate
0 ImagesCat. No.: HY-115619EPZ004777 formate is an effective and selective DOT1L inhibitor, with IC50 being 0.4 nM. EPZ004777 formate reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 formate selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 formate can be used for the study of leukemia.
-
PRMT5-IN-50
0 ImagesCat. No.: HY-172732CAS No.: 3002409-47-1PRMT5-IN-50 is an orally active and selective inhibitor of PRMT5. PRMT5-IN-50 has good metabolic stability and low clearance rate in human liver microsomes. PRMT5-IN-50 inhibits SDMA/HCT116-MTAPdel and SDMA/HCT116-MTAPwt with IC50s value of 1.0, 536 nM for arginine symmetric methylation, 19, 1620 nM for anti-proliferation, respectively. PRMT5-IN-50 inhibits tumor growth in mice.
-
PRMT1-IN-1
0 ImagesCat. No.: HY-115758CAS No.: 1025948-98-4PRMT1-IN-1 is a PRMT1 inhibitor.
-
PRMT5-IN-10
0 ImagesCat. No.: HY-139823CAS No.: 2567564-23-0PRMT5-IN-10 has promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex.
-
NSD3-IN-1
0 ImagesCat. No.: HY-142093CAS No.: 347340-51-6NSD3-IN-1 (compound B1) is an inhibitor of histone methyltransferase NSD3 with an IC50 value of 28.58 μM.
-
PRMT5-IN-33
0 ImagesCat. No.: HY-162230CAS No.: 3054228-62-2
-
D595
0 ImagesCat. No.: HY-117542CAS No.: 16740-29-7D595 is a phenylethylamine calcium channel blocker with potent negative inotropic activity. D595 has shown significant efficacy in its corresponding pharmacological studies, especially in inhibiting the uptake of monoamine neurotransmitters. D595 has high affinity in binding to the dopamine transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET). Structural adjustments of D595, especially changes in the hydroxyl stereochemistry, significantly affect its interaction with the transporters, showing a specific preference for stereoisomers.
-
SJY26
0 ImagesCat. No.: HY-178485SJY26 is a PI3K/HDAC dual-target inhibitor with IC50s of 0.59 nM (PI3Kα and PI3Kδ), 2.02 nM (PI3Kγ), 12.69 nM (PI3Kβ) and 114 nM (HDAC1). SJY26 exhibits potent broad-spectrum anti-proliferative activity, and is particularly sensitive to Jurkat and PC9R cells. SJY26 inhibited the migration of PC9R cells, arrested the cell cycle and induced cell apoptosis. SJY26 reduces AKT phosphorylation, and decreases histone H3 deacetylation (Ac-H3). SJY26 can be used for the studies of non-small cell lung cancer and leukemia.
-
MS2928
0 ImagesCat. No.: HY-181849MS2928 is a selective SETD8 inhibitor with an IC50 of 0.14 μM against SETD8 methyltransferase activity. MS2928 reduces cellular H4K20me1 levels and inhibits proliferation of SETD8-overexpressing multiple myeloma cells. MS2928 inhibits tumor growth in xenograft mouse models of SETD8-overexpressing multiple myeloma. MS2928 can be used for the study of SETD8 biological functions and multiple myeloma.
-
EPZ028862
0 ImagesCat. No.: HY-145444CAS No.: 1887082-53-2
-
GSK2807
0 ImagesCat. No.: HY-104009CAS No.: 2245255-65-4
-
LSD1-IN-32
0 ImagesCat. No.: HY-161869LSD1-IN-32 (compound 11e) is a potent LSD1 inhibitor with an IC50 value of 0.99 µM. LSD1-IN-32 inhibits RANKL-induced osteoclastogenesis, bone resorption and F-actin belt formation. LSD1-IN-32 has the potential for the research of osteoporosis.
-
PROTAC IKZF3 degrader-1
0 ImagesCat. No.: HY-172368PROTAC IKZF3 degrader-1 is a potent dual-targeting agent that functions as both a CARM1 inhibitor (IC50 = 2 nM) and a CRBN-dependent PROTAC degrader of IKZF3. PROTAC IKZF3 degrader-1 simultaneously inhibits CARM1 activity (reducing BAF155 methylation) and recruits CRBN to induce the targeted degradation of IKZF1, IKZF3, ZFP91, and FGD3 proteins; this leads to the downregulation of oncogenes, more potent induction of apoptosis, and the overcoming of immunomodulatory imide drugs resistance. PROTAC IKZF3 degrader-1 is suitable for research into both IMiD-sensitive and IMiD-resistant multiple myeloma.
-
DC541
0 ImagesCat. No.: HY-182676CAS No.: 2606862-00-2DC541 (Compound 20) is a selective NTMT1 inhibitor with an IC50 of 0.34 μM. DC541 reduces the level of me3-RCC1 in colorectal cancer cells. DC541 is applicable to research related to colorectal cancer.
-
PRMT5-IN-21
0 ImagesCat. No.: HY-150081CAS No.: 2922673-38-7PRMT5-IN-21 (compound 1) is a potent cyclonucleoside PRMT5 inhibitor.
-
PRMT5-IN-36-d3
0 ImagesCat. No.: HY-163591CAS No.: 3034034-10-8PRMT5-IN-36-d3 is the deuterated derivative of PRMT5-IN-36. PRMT5-IN-36-d3 (compound 4) is an orally active PRMT5 inhibitor for cancer research.
