Histone Methyltransferase

Methyltransferase

Histone Methyltransferase

Related Products

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 Isoform Comparison

Histone Methyltransferase Related Products (461)
Antibodies (84)
Histone Methyltransferase Isoform Comparison

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By Effects:	Controls (6) Ligand (1) Inhibitors (394) Agonist (1) Degraders (12) Antagonists (8) Activators (2) Modulators (2) Chemicals (2) Inducer (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-156680

TNG-462	Inhibitor	99.91%
TNG-462 is an orally active and selective PRMT5 inhibitor with anti-tumor activity against methylthioadenosine phosphorylase (MTAP) deficiency and/or methylthioadenosine (MTA) accumulation cancers.

HY-101925

CM-272	Inhibitor	98.70%
CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC₅₀s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death.

HY-112445

SGC3027	Inhibitor	98.06%
SGC3027 is a histone methyltransferase inhibitor. SGC3027 is the first potent, selective and cell active chemical probe for PRMT7.

HY-100034

NSC 663284	Inhibitor	99.29%
NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC₅₀ for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 inhibits NSD2 (IC₅₀ of 170 nM) through a direct interaction with the catalytic SET domain (K_d of 370 nM).

HY-101512

A-395	Inhibitor	99.12%
A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC₅₀ of 18 nM.

HY-107777

LLY-283	Inhibitor	99.22%
LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC₅₀ of 22 nM and a K_d of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity.

HY-148419

Ralometostat	Inhibitor	98.89%
TNG908 is a MTAP synergistic PRMT5 inhibitor. TNG908 crosses the blood-brain barrier and is orally active. TNG908 could be used in cancer research.

HY-18962

AMI-1	Inhibitor	≥98.0%
AMI-1 is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC₅₀s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 exerts PRMTs inhibitory effects by blocking peptide-substrate binding.

HY-18627A

PFI-2 hydrochloride	Inhibitor	99.48%
PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC₅₀ value of 2.0 nM and (S)-PFI-2 shows inhibiting activity with IC₅₀ value of 1.0 μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis.

HY-150190

F5446	Inhibitor	99.38%
F5446 (Compound 1) is a selective small molecule inhibitor of SUV39H1 methyltransferase. F5446 decreases H3K9me3 deposition at the FAS promoter, increases Fas expression and increases colorectal carcinoma cell sensitivity to FasL-induced apoptosis in vitro. F5446 suppresses human colon tumor xenograft growth in vivo.

HY-12970

EPZ020411	Inhibitor	98.07%
EPZ020411 is a selective inhibitor of PRMT6 with an IC₅₀ of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 can be used for the research of cancer.

HY-109108A

Valemetostat tosylate	Inhibitor	99.84%
Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC₅₀ values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma.

HY-116522

AR420626		98.29%
AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3) (IC₅₀=117 nM). AR420626 has anti-inflammatory, anticancer and antidiabetic activities. AR420626 improves neurogenic diarrhea by inhibiting nAChR mediated neural pathways. AR420626 inhibits the growth of HepG2 xenografts and inhibits the proliferation of hepatoma cells by inducing apoptosis. AR420626 also suppresses allergic asthma and eczema and has the ability to activate GPR41 to increase Ca²⁺ signal-mediated glucose uptake and improve diabetes.

HY-103663

MAK683	Inhibitor	99.18%
MAK683 is an embryonic ectoderm development (EED) inhibitor extracted from patent US20160176882 A1, compound example 2. MAK683 exhibits IC₅₀s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay.

HY-141429A

AS-99 TFA	Inhibitor	99.15%
AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC₅₀= 0.79 μM, K_d= 0.89 μM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.

HY-B1322A

Amodiaquine	Inhibitor	99.98%
Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect.

HY-130708

UNC6852	Inhibitor	99.09%
UNC6852 is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a von Hippel-Lindau ligand, with an IC₅₀ of 247 nM for EED.

HY-139626

EPZ-719	Inhibitor	99.85%
EPZ-719 is a selective, orally effective SETD2 inhibitor with an IC₅₀ value of 0.005 μM. EPZ-719 has anticancer activity.

HY-15226

AZ505	Inhibitor	99.99%
AZ505 is a potent and selective SMYD2 inhibitor with an IC₅₀ of 0.12 μM.

HY-12970A

EPZ020411 hydrochloride	Inhibitor	98.15%
EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC₅₀ of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer.

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