About 30 results found for searched term "Histone Methyltransferase" (0.12 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M2024 | BIX 01294 Trihydrochloride | Histone Methyltransferase |
| BIX 01294 Trihydrochloride is a potent inhitor of G9a histone methyltransferase with IC50 of 2.7 μM. | ||
| M2179 | EPZ-5676 | Histone Methyltransferase |
| Pinometostat | ||
| EPZ-5676 is a potent and selective aminonucleoside inhibitor of DOT1L histone methyltransferase. | ||
| M2736 | GSK343 | EZH2 |
| GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. | ||
| M3101 | UNC0224 | Histone Methyltransferase |
| UNC0224 is a selective histone lysine methyltransferase (HMTase) inhibitor for G9a and GLP with IC50 of 15 nM and 20 nM, respectively. | ||
| M3103 | UNC0631 | Histone Methyltransferase |
| UNC0631 is a selective histone lysine methyltransferase (HMTase) inhibitor for G9a and GLP with IC50 of 6 nM and 15 nM, respectively, with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity. | ||
| M3105 | UNC0646 | Histone Methyltransferase |
| UNC0646 is a selective histone lysine methyltransferase (HMTase) inhibitor for G9a and GLP with IC50 of 6 nM and 15 nM , respectively, with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity. | ||
| M3783 | C7280948 | PRMTs |
| C7280948 is an inhibitor of histone arginine methyltransferase PRMT1 with IC50 values of 12.75 uM. | ||
| M6312 | LLY-283 | PRMTs |
| LLY-283 is the potent and selective SAM-competitive chemical probe for PRMT5. It inhibits PRMT5 enzyme activity with IC50 of 20 nM for methylation of an H4R3 derived peptide substrate, and shows greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. | ||
| M6336 | 3-Deazaneplanocin A hydrochloride | Histone Methyltransferase |
| DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride | ||
| 3-Deazaneplanocin A hydrochloride（DZNep HCl） is a eZH2 histone methyltransferase inhibitor. | ||
| M6362 | A 196 | Histone Methyltransferase |
| A-196 is a potent selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively, and biochemically inhibits SUV4-20 in a substrate-competitive manner. In addition, A-196 is a first-in-class chemical probe for SUV4-20, which can be used to study the role of histone methyltransferases in genome integrity. | ||
| M6592 | Chaetocin | Histone Methyltransferase |
| Chaetocin is a specific inhibitor of the histone methyltransferase (HMT) SU(VAR)3-9 with an IC50 of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase (TrxR) with an IC50 of 4 μM. | ||
| M7509 | UNC0642 | Histone Methyltransferase |
| UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels. | ||
| M8397 | BRD4770 | Histone Methyltransferase |
| BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 inhibited the dimethylation and trimethylation of H3K9, EC50 was 5 µM, and had little effect on H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 activates the ataxic telangiectasia mutation (ATM) pathway and induces cell senescence. | ||
| M8529 | A-366 | Histone Methyltransferase |
| A366 | ||
| A-366 is a potent and highly selective peptide-competitive inhibitor of histone methyltransferase G9a, with IC50s of 3.3 nM and 38 nM for G9a and GLP, respectively, and is more than 1,000-fold selective for G9a and GLP over 21 other methyltransferases. A-366 is also a potent inhibitor of Spindlin1-H3K4me3 interaction (IC50=182.6 nM).A-366 shows high affinity for human H3R (Ki=17 nM) and exhibits subtype selectivity between subpopulations of the histaminergic and dopaminergic receptor families. It can be used for induction and maintenance of pluripotent stem cells in mice. | ||
| M10860 | MRK-740 | Histone Methyltransferase |
| MRK-740 is a potent, selective, substrate-competitive PRDM9 histone methyltransferase inhibitor,IC50 80 nM. MRK-740 is more selective to PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 Reduces PRDM9-Dependent H3K4 Trimethylation (IC50 0.8 μM). | ||
| M13843 | BRD9539 | Histone Methyltransferase |
| BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1. | ||
| M13850 | SGC3027 | Histone Methyltransferase |
| SGC3027 is a histone methyltransferase inhibitor. SGC3027 is the first potent, selective and cell active chemical probe for PRMT7. | ||
| M20492 | AMI-1, free acid | Histone Methyltransferase |
| AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively. | ||
| M21329 | Histone H2A (1-20) | Peptides |
| Histone H2A (1-20) is a 35 amino acid histone H2A peptide fragment that is a substrate for methyltransferase/demethylase enzymes. Sequence: Ser-Gly-Arg-Gly-Lys-Gln-Gly-Gly-Lys-Ala-Arg-Ala-Lys-Ala-Lys-Thr-Arg-Ser-Ser-Arg. | ||
| M21504 | AS-99 free base | Histone Methyltransferase |
| AS-99 is the first-in-class, effective and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemia activity. | ||
| M21505 | AS-99 | Histone Methyltransferase |
| AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with antileukemic activity. | ||
| M21507 | AS-99 TFA | Histone Methyltransferase |
| AS-99 TFA is the first-in-class, effective and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemia activity. In vivo, AS-99 TFA blocked cell proliferation, induced apoptosis and apoptosis, down-regulated MLL fusion target genes, and alleviated leukaemia. | ||
| M21676 | EPZ-719 | Histone Methyltransferase |
| EPZ719 | ||
| EPZ-719 is a First-in-Class, novel and potent SET domain-containing protein 2 (SETD2) inhibitor (IC50 = 0.005 μM), with a high selectivity over other histone methyltransferases. | ||
| M29869 | DC-S239 | Histone Methyltransferase |
| DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC50 value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity. | ||
| M30844 | CPUY074020 | Histone Methyltransferase |
| CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity. | ||
| M38950 | Tanshindiol C | Histone Methyltransferase |
| Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. | ||
| M40717 | UNC0321 | Histone Methyltransferase |
| UNC0321 is a high affinity inhibitor of GPCRs and can be used in studies related to chromatin remodeling. It is also a selective inhibitor of histone methyltransferase G9a with a Ki of 63 pM and an IC50 value of 6-9 nM.In addition, UNC0321 also inhibits GLP with an IC50 value of 15-23 nM. | ||
| M41686 | BBDDL2059 | Histone Methyltransferase |
| BBDDL2059 is a selective covalent inhibitor of histone methyltransferase EZH2 with an IC50 of 1.5 nM for EZH2-Y641F. | ||
| M45100 | KDM2A/7A-IN-1 | Histone demethylase |
| KDM2A/7A-IN-1 is a first-in-class, selective, cell-permeable inhibitor of the histone lysine demethylase KDM2A/7A, with an IC50 value of 0.16 μM for KDM2A, 75-fold more selective than other JmjC lysine demethylases, and with no effect on methyltransferases or histone acetyltransferases. KDM2A was 75 times more selective than other JmjC lysine demethylases and had no effect on methyltransferases and histone acetyltransferases. | ||
| M50975 | Histone H3 (21-44) | Others |
| Histone H3 (21-44), derived from histone H3 21-44 amino acids, is usually used as a substrate (such as protein arginine methyltransferases) for methylation assays. | ||
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