Histone modifications are essential for controlling both overall gene expression and stage-specific gene expression. While histones H3K9 and H3K27 are typically associated with gene repression, methylation on histones H3K4, H3K36, and H3K79 is typically associated with gene activation. Site-specific methyltransferases and demethylases dynamically control the methylation of histone lysines. The methylation of H3K27 in cells is carried out by EZH2 (the catalytic subunit of PRC2).
Inhibiting DOT1L, a histone H3 lysine 79 methyltransferase, improves the production of induced pluripotent stem cells (iPSCs). A powerful and specific DOT1L inhibitor, EPZ-5676.
The histone methyltransferase enhancer of zeste homolog 2 (EZH2) trimethylates histone 3's lysine 27 (H3K27me3), which results in chromatin condensation and transcriptional repression and is essential for PRC2 activity.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V51586 | PRMT5-IN-29 | 2242788-69-6 | PRMT5-IN-29 is a potent orally bioactive PRMT5 inhibitor (antagonist) with IC50 of 1.5 μM. |
|
V56090 | PRMT5-IN-30 | 330951-01-4 | PRMT5-IN-30 (compound 17) is a potent and specific protein arginine methyltransferase 5 (PRMT5) inhibitor (antagonist) with IC50 of 0.33 μM and a Kd of 0.987 μM. |
|
V79681 | PRMT5-IN-31 | PRMT5-IN-31 (Compound 3m) is a selective PRMT5 inhibitor (IC50= 0.31 μM). | |
|
V75867 | PRMT5-IN-32 | 2918815-34-4 | PRMT5-IN-32 is an inhibitor (blocker/antagonist) of PRMT5. |
|
V51593 | PRMT5-IN-4 | 152615-84-4 | PRMT5-IN-4 (compound AAA-1) is an inhibitor (blocker/antagonist) of PRMT5. |
|
V51595 | PRMT5-IN-9 | 2691869-52-8 | PRMT5-IN-9 is a novel PRMT5 inhibitor for cancer research with IC50 of 0.01 μM. |
|
V51588 | PRMT6-IN-3 | 2890765-10-1 | PRMT6-IN-3 (compound 25) is a selective PRMT6 conjugate with IC50 of 192 nM. |
|
V78745 | RK-0133114 | RK-0133114 is a G9a inhibitor and the R-enantiomer of RK-701. | |
|
V38321 | RK-701 | 2648855-18-7 | RK-701 is a selective and non-genotoxic inhibitor of G9a with IC50 of 23-27 nM. |
|
V79839 | SETD7-IN-1 | SETD7-IN-1 (compound 7) is an analog of PFI-2. | |
|
V36917 | SETDB1-TTD-IN-1 | 2755823-12-0 | SETDB1-TTD-IN-1 is a specific and endogenous binder-competitive inhibitor of SETDB1-TTD with a Kd of 88 nM. |
|
V0399 | SGC 0946 | 1561178-17-3 | SGC 0946 (SGC-0946; SGC0946) is a potent and selective inhibitor of DOT1L (DOT1 Like Histone Lysine Methyltransferase)with antineoplastic activity. |
|
V2763 | SGC2085 | 1821908-48-8 | SGC2085, identified fromvirtual screening approaches, is a novel, potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50of 50 nM. |
|
V2107 | SGC2085 HCl | 1821908-49-9 | SGC2085 HCl, identified fromvirtual screening approaches, is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50of 50 nM. |
|
V0383 | SGC707 | 1687736-54-4 | SGC707 (SGC-707) is a novel, cell-permeable and allosteric PRMT3 inhibitor (protein arginine methyltransferase 3 inhibitor) with potential anticancer activity. |
|
V3457 | Sinefungin | 58944-73-3 | Sinefungin (Adenosyl-Ornithine, Antibiotic 32232RP, A-9145) is a 5′-aminoalkyl analog of SAH and a natural product from cultures of Streptomyces incamatus and S. |
|
V56087 | SKF 91488 dihydrochloride (Homodimaprit dihydrochloride) | 68941-21-9 | SKF 91488 di-HCl (Homodimaprit) is a potent, noncompetitive histamine N-methyltransferase inhibitor (antagonist) with a Ki of 0.9 microM. |
|
V76461 | SW2_110A | SW2_110A is a selective chromobox 8 chromodomain (CBX8 ChD) inhibitor (antagonist) with a Kd of 800 nM. | |
|
V35222 | Tanshindiol C | 97465-71-9 | Tanshindiol C is an S-adenosylmethionine competitive EZH2 (Histone Methyltransferase) inhibitor (antagonist) with IC50 of 0.55 μM for inhibiting methyltransferase activity. |
|
V0382 | Tazemetostat (EPZ6438; E-7438) | 1403254-99-8 | This product is discontinued due to commercial reason. |
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