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
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PRMT7
(8)
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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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EZH2 ligand-5
0 ImagesCat. No.: HY-W1063360CAS No.: 2225940-27-0
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EZH2-IN-19
0 ImagesCat. No.: HY-163741CAS No.: 3026848-13-2
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PROTAC EZH2 Degrader-40
0 ImagesCat. No.: HY-181409CAS No.: 3093642-40-8PROTAC EZH2 Degrader-40 (compound 56) is a PROTAC protein degrader targeting EZH2 with an IC50 of 15.35 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-40 can be used for the research of diffuse large B-cell lymphoma.
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CBX2-IN-1
0 ImagesCat. No.: HY-181089CAS No.: 3124602-03-2CBX2-IN-1 is a CBX2 inhibitor with an IC50 of 9.6 μM. CBX2-IN-1 binds the CBX2 chromodomain’s H3K27me3 binding channel, blocks interaction between CBX2 and H3K27me3, and exhibits selective affinity toward CBX2, CBX4, CBX6, CBX7, and CBX8 over CBX1, CBX3, and CBX5. CBX2-IN-1 can be used for the research of prostate cancers.
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AZD3632
0 ImagesCat. No.: HY-182793CAS No.: 3058433-50-1Synonyms: MLL1-IN-1AZD3632 (MLL1-IN-1) is an orally active MLL1 inhibitor with an IC50 of 0.043 μM. AZD3632 induces Menin protein degradation and inhibits the proliferation of leukemia cells. AZD3632 can induce tumor regression in leukemia-bearing mice. AZD3632 is useful for research into MLL1-associated leukemia.
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PRMT5-IN-53
0 ImagesCat. No.: HY-178028CAS No.: 3113303-04-8PRMT5-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC50s of ≥ 9.7 against hPRMT5 and mPRMT5. PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. PRMT5-IN-53 effectively inhibits PRMT5 locally in the intestines of mice, significantly reducing the number and area of polyps, while avoiding systemic hematological toxicity (such as anemia, neutropenia). PRMT5-IN-53 can be used for the study of colorectal cancer especially for familial adenomatous polyposis (FAP).
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MU1656
0 ImagesCat. No.: HY-145813CAS No.: 2766698-38-6MU1656 is a potent and selective inhibitor of histone methyltransferase DOT1L, with an IC50 of 2 nM. MU1656 can be used for the research of hematological malignancies.
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SGC2085 hydrochloride
0 ImagesCat. No.: HY-100565ACAS No.: 1821908-49-9SGC2085 hydrochloride is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 hydrochloride also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins.
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UNC7242
0 ImagesCat. No.: HY-181914UNC7242 is an antagonist that binds to the Tudor domains of PHF1 and PHF19, with a Kd of 1.13 μM for PHF1 and 0.64 μM for PHF19. UNC7242 fails to displace full-length PHF1 or PHF19 from H3K36me3 nucleosomes or chromatin. UNC7242 can be used in studies related to multiple myeloma, endometrial stromal sarcoma, and ossifying fibromyxoid tumor.
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NSD3-IN-2
0 ImagesCat. No.: HY-142094CAS No.: 675190-57-5NSD3-IN-2 is a potent NSD3 inhibitor with an IC50 value of 17.97 μM. NSD3-IN-2 inhibits the growth and proliferation of non-small cell lung cancer cell lines H460, H1299 and H1650 with anti-cancer activity.
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YZ-17
0 ImagesCat. No.: HY-189213YZ-17 is a PROTAC degrader targeting PRMT5, with DC50 = 2.2 μM (HCC1806 cells). YZ-17 recruits CRBN E3 ligase and induces PRMT5 degradation through the ubiquitin-proteasome system, inhibiting PRMT5-mediated symmetric dimethylarginine modification. YZ-17 co-degrades the PRMT5 adaptor protein MEP50 via a CRBN-dependent mechanism. YZ-17 induces G1 phase cell cycle arrest and inhibits colony formation in cancer cells. YZ-17 exhibits antiproliferative activity in various cancer cells. YZ-17 shows antitumor efficacy in a triple-negative breast cancer xenograft mouse model. YZ-17 can be used for research on triple-negative breast cancer.
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SKLB-03220
0 ImagesCat. No.: HY-177497CAS No.: 2852050-29-2SKLB-03220 is a selective and orally active EZH2 covalent inhibitor with an IC50 of 1.72 nM for EZH2MUT. SKLB-03220 exhibits weak activities against other tested histone methyltransferases (HMTs) and kinases. SKLB-03220 displays noteworthy potency against ovarian cancer cell lines and induces cell apoptosis. SKLB-03220 significantly inhibits tumor growth in PA-1 xenograft model. SKLB-03220 can be used for the study of ovarian cancer.
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Go 6983 (GMP)
0 ImagesCat. No.: HY-13689GCAS No.: 133053-19-7Go 6983 GMP is Go 6983 (HY-13689) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Go 6983 is a dual inhibitor targeting Suv39h1/2 (KMT1A/KMT1B) and PKC, as well as a transcriptional activator capable of inducing DNA hypomethylation. Go 6983 stimulates the transcription of Prdm14 by reducing Suv39h1/2 protein levels, decreasing histone modifications in the Prdm14 promoter region, and increasing the recruitment of RNA polymerase II. Go 6983 induces genome-wide DNA hypomethylation by inhibiting de novo methyltransferase expression and increasing Tet1/Tet2 levels, thereby promoting self-renewal and pluripotency maintenance of stem cells. Meanwhile, Go 6983 can block PKC-mediated signaling pathways to reduce the expression of EMT-related genes and eliminate the upregulation of antioxidant genes downstream of NRF2. Go 6983 is mainly used in mechanism studies related to myocardial ischemia/reperfusion injury.
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PRMT5-IN-58
0 ImagesCat. No.: HY-189289CAS No.: 3107304-24-2PRMT5-IN-58 is an MTA-cooperative PRMT5 inhibitor and PRMT5-MTA complex binder (IC50 = 11.7 nM) that inhibits methyltransferase activity and SDMA (HY-101410) production by stabilizing the MTA-bound conformation, and induces apoptosis via sub-G1 phase accumulation, exhibiting selective antiproliferative activity against MTAP-deleted cancer cells over MTAP wild-type cells. PRMT5-IN-58 can be used for research on MTAP-deleted cancers.
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RK-0080552
0 ImagesCat. No.: HY-172614CAS No.: 313527-11-6Synonyms: RK-552RK-0080552 (RK-552) is a NSD2 inhibitor with an IC50 of 0.11 μM, and it exhibits selectivity over histone methyltransferases G9a (IC50: 1.2 μM) and SET7/9 (IC50: >50 μM). RK-0080552 functionally inhibits NSD2 histone methyltransferase activity, reduces the dimethylation level of histone H3 lysine 36, suppresses IRF4 transcription, induces apoptosis and triggers cell death. RK-0080552 inhibits the growth of xenograft tumors and prolongs host survival. RK-0080552 is available for the research of multiple myeloma.
