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
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Histone Methyltransferase
(368)
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EZH1
(11)
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EZH2
(85)
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DOT1L
(21)
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SMYD2
(9)
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SMYD3
(9)
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SUV39H2/
KMT1B (4)View all products
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EHMT2/
G9a/ (32)KMT1C View all products
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EHMT1/
GLP/ (20)KMT1D View all products
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ASH1L/
KMT2H (4)View all products
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SETDB1/
KMT2G (4)View all products
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SETD2/
KMT3A (5)View all products
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NSD2/
MMSET/ (16)WHSC1 View all products
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NSD3/
WHSC1L1 (4)View all products
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SETD7/
KMT7 (6)View all products
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SETD8/
KMT5A (5)View all products
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PRMT1
(25)
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PRMT3
(17)
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PRMT4
(19)
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PRMT5
(64)
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PRMT6
(23)
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PRMT7
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PRMT8
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All Product Categories
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Histone Methyltransferase Inhibitors
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Histone Methyltransferase Agonists
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Histone Methyltransferase Antagonists
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Histone Methyltransferase Activators
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Histone Methyltransferase Modulators
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Histone Methyltransferase Chemical
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Histone Methyltransferase Inducers
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Histone Methyltransferase Degraders
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Histone Methyltransferase Controls
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Histone Methyltransferase Ligands
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Histone Methyltransferase Related Products (687)
Related Products (687)
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Antibodies (84)
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Histone Methyltransferase Isoform Comparison
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PROTAC EZH2 Degrader-29
0 ImagesCat. No.: HY-181357CAS No.: 3093642-30-6PROTAC EZH2 Degrader-29 (compound 66) is a is a PROTAC protein degrader targeting EZH2 with an IC50 of 24.53 μM against diffuse large B-cell lymphoma cells. PROTAC EZH2 Degrader-29 can be used in studies related to diffuse large B-cell lymphoma.
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MS1262 TFA
0 ImagesCat. No.: HY-176036APurity: 99.32%MS1262 TFA is a blood-brain barrier-permeable, selective inhibitor of histone methyltransferases G9a (EHMT2) and GLP (EHMT1), with an IC50 of 19 nM and a Kd of 74 nM against G9a, and an IC50 of 6 nM and a Kd of 19 nM against GLP. MS1262 TFA reduces the dimethylation level of histone H3 lysine 9 and decreases the size of Aβ plaques. MS1262 TFA restores hippocampal long-term potentiation (LTP) and miniature excitatory postsynaptic current (sEPSC) frequency, ameliorates spatial memory deficits, and reverses anxiety-like and depression-like behaviors in AD model mice. MS1262 TFA reverses the expression/phosphorylation levels of early AD biomarkers, providing support for stage-specific diagnosis of AD. MS1262 TFA reduces the risk of thrombus rupture. MS1262 TFA can be used in research related to Alzheimer's disease, colorectal cancer, and triple-negative breast cancer.
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5-Octyl-α-ketoglutarate
0 ImagesCat. No.: HY-145452CAS No.: 1616344-00-3Synonyms: 5-Octyl 2-oxopentanedioate5-Octyl-α-ketoglutarate (5-Octyl 2-oxopentanedioate) is a cell-permeable substrate for lysine demethylase. 5-Octyl-α-ketoglutarate is related to protein demethylation, inhibits cell proliferation of wtCRBN expressing cells, and also enhances Lenalidomide (HY-A0003)-induced sensitivity and inhibits myeloma (MM) ) drug resistance of cells. When myeloma (MM) cells undergo glutamine-dependent proliferation, α-ketoglutarate increases glutamine catabolism to promote protein demethylation.
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PRMT5-IN-51
0 ImagesCat. No.: HY-176231CAS No.: 3064668-92-1PRMT5-IN-51 (compound 16–19F) is a potent PRMT5 inhibitor. PRMT5-IN-51 shows antiproliferative activity.
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ZL-28-6
0 ImagesCat. No.: HY-158157CAS No.: 2739807-18-0ZL-28-6 is a type I PRMT inhibitor (IC50: 18 nM). ZL-28-6 effectively targets CARM1 (a member of PRMT) within cells and can be used for cancer research.
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PRMT5 ligand 1
0 ImagesCat. No.: HY-173092CAS No.: 1616393-25-9PRMT5 ligand 1 (compound 3) is the ligand for PRMT5 that can be used as target protein ligand for synthesis of PROTAC degrader MS4322 (HY-141877).
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Flavokawain A (Standard)
0 ImagesFlavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.
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TC-E 5003 (Standard)
0 ImagesCat. No.: HY-107574RCAS No.: 17328-16-4TC-E 5003 (Standard) is the analytical standard of TC-E 5003 (HY-107574). This product is intended for research and analytical applications. TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein Kinase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers.
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Setin-1
0 ImagesCat. No.: HY-118715CAS No.: 1313802-67-3Setin-1 is one of the most potent inhibitors of Set7, acting by inhibiting KMTase G9a.
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SETDB1-IN-1
0 ImagesCat. No.: HY-185849CAS No.: 2585194-96-1SETDB1-IN-1 is a SETDB1 inhibitor with an IC50 of 16 μM. SETDB1-IN-1 inhibits histone methyltransferase) activity via SAM-competitive and peptide-dependent mechanisms. SETDB1-IN-1 is applicable to research related to melanoma, lung cancer, liver cancer, breast cancer and prostate cancer.
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EPZ0025654
0 ImagesCat. No.: HY-117927CAS No.: 1888328-89-9Synonyms: GSK3536023EPZ0025654 (GSK3536023) is an inhibitor for protein arginine methyltransferases 4 (PRMT4) (which is also known as coactivator associated arginine methyltransferase 1 CARM1), with IC50 of 3 nM.
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EHMT2-IN-1 (Standard)
0 ImagesCat. No.: HY-111778RCAS No.: 2230849-55-3EHMT2-IN-1 (Standard) is the analytical standard of EHMT2-IN-1 (HY-111778). This product is intended for research and analytical applications. EHMT2-IN-1 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disorder or cancer.
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CMP-5 dihydrochloride
0 ImagesCat. No.: HY-113846ACAS No.: 2309409-79-6CMP-5 dihydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 dihydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 dihydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected.
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KAT-IN-2
0 ImagesCat. No.: HY-165496CAS No.: 164789-02-0KAT-IN-2 (7) is a potent and selective kynurenine aminotransferase II (KATII) inhibitor.
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HH2853
0 ImagesCat. No.: HY-187629CAS No.: 2202678-04-2HH2853 is an orally active EZH1/EZH2 inhibitor, with an IC50 of 9.26 nM for EZH1 and IC50 values ranging from 2.21 to 3.75 nM for both wild-type and mutant EZH2. HH2853 simultaneously inhibits the methyltransferase activities of EZH1 and EZH2, blocks the compensatory pathway that arises following EZH2 inhibition, and reduces H3K27me3 levels. HH2853 upregulates the expression of c-Myc and TfR-1 to induce intracellular iron accumulation, and stabilizes GPX4 via HSPA5 to suppress ferroptosis. HH2853 combined with Erastin (HY-15763) synergistically inhibits EZH2 wild-type DLBCL cell proliferation. HH2853 alone shows weak activity against EZH2 wild-type DLBCL and is well tolerated. HH2853 is applicable for research related to diffuse large B-cell lymphoma, non-Hodgkin's lymphoma, epithelioid sarcoma, and follicular lymphoma.
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SGC2085 (Standard)
0 ImagesCat. No.: HY-100565RCAS No.: 1821908-48-8SGC2085 (Standard) is the analytical standard of SGC2085 (HY-100565). This product is intended for research and analytical applications. SGC2085 is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins.
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UNC0224 (Standard)
0 ImagesCat. No.: HY-10929RCAS No.: 1197196-48-7UNC0224 (Standard) is the analytical standard of UNC0224 (HY-10929). This product is intended for research and analytical applications. UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 2.6 nM, an IC50 of 15 nM and a Kd of 23 nM. UNC0224 also potently inhibits b>GLP with assay-dependent IC50 values of 20-58 nM. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E.
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Pemrametostat succinate
0 ImagesCat. No.: HY-101563ACAS No.: 1848944-46-6Synonyms: GSK3326595 succinate; EPZ015938 succinateGSK3326595 succinate (EPZ015938 succinate) is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 succinate decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 succinate can be used for research of relapsed/refractory mantle cell lymphoma.
