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 |
|---|---|---|---|---|
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V4503 | Onametostat (JNJ-64619178) | 2086772-26-9 | Onametostat (JNJ-64619178; JNJ64619178) is a novel, potent, selective and pseudo-irreversiblePRMT5(protein arginine methyltransferase 5) inhibitor with potential anticancer activity. |
|
V76673 | OTS186935 hydrochloride | OTS186935 HCl is a potent inhibitor of protein methyltransferase SUV39H2 with IC50 of 6.49 nM. | |
|
V0397 | PFI-2 | 1627676-59-8 | PFI-2 (PFI2) is a novel, potent and selective inhibitor of lysine methyltransferase SETD7 [SET domain containing (lysine methyltransferase) 7] with anticancer activity. |
|
V2548 | PFI-2 HCl | 1627607-87-7 | PFI-2 HCl, the hydrochloride salt of PFI-2, is a selective, and cell-active lysine methyltransferase SETD7 inhibitor with potential antitumor activity. |
|
V0378 | Pinometostat (EPZ-5676) | 1380288-87-8 | Pinometostat (formerly EPZ 5676) is a potent and SAM (S-adenosyl methionine) competitive DOT1L protein methyltransferase (PMT) inhibitor with potential antitumor activity. |
|
V75861 | Pociredir (FTX-6058) | 2490676-18-9 | Pociredir (FTX-6058) is a potent, orally bioactive inhibitor of embryonic ectodermal development (EED). |
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V40993 | Pociredir hydrochloride (FTX-6058 hydrochloride) | 2490676-19-0 | Pociredir (FTX-6058) HCl is a potent, orally bioactive inhibitor of embryonic ectoderm development (EED). |
|
V79232 | PRMT4-IN-3 | PRMT4-IN-3 (compound 56) is a potent inhibitor of class I protein arginine methyltransferase (PRMT), targeting PRMT4 (IC50= 37 nM) and PRMT4 (IC50= 253 nM). | |
|
V51594 | PRMT5-IN-1 | 2366149-83-7 | PRMT5 IN-1, a hemiaminal, is a potent conjugated protein protamine methyltransferase 5 (PRMT5) dye, inhibiting PRMT5/MEP50 with IC50 of 11 nM. |
|
V51585 | PRMT5-IN-10 | 2567564-23-0 | PRMT5-IN-10 has a good structure-dependent inhibitory activity against the protein methyltransferase PRMT5:MEP50 complex. |
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V51587 | PRMT5-IN-11 | 2567564-33-2 | PRMT5-IN-11 is a compound that can inhibit the protein methyltransferase PRMT5:MEP50 complex in a structure-dependent manner in the (sub)micromolar range. |
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V51589 | PRMT5-IN-12 | 2568927-94-4 | PRMT5-IN-12 has significant inhibitory activity against PRMT5. |
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V51592 | PRMT5-IN-13 | 2376795-15-0 | PRMT5-IN-13 is a selective protein arginine methyltransferase 5 (prmt5) inhibitor. |
|
V51598 | PRMT5-IN-14 | 2278356-90-2 | PRMT5-IN-14 is a PRMT5 inhibitor used to study cancer, sickle cell and inherited persistent fetal hemoglobin (HPFH) mutations. |
|
V51591 | PRMT5-IN-15 | 2410637-87-3 | PRMT5-IN-15 is a PRMT5 inhibitor (antagonist) with IC50 of 0.84 nM. |
|
V51584 | PRMT5-IN-19 | 2783961-86-2 | PRMT5-IN-19 (Compound 41) is an epidermally active, non-nucleoside PRMT5-selective with IC50s of 23.9 nM (radiobiochemical assay), 47 nM (AlphaLISA assay). |
|
V51597 | PRMT5-IN-22 | PRMT5 inhibitor | |
|
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V51596 | PRMT5-IN-23 | PRMT5-IN-23 (compound 50) is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor (antagonist) with anti-tumor activity. | |
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V75868 | PRMT5-IN-27 | 2790567-82-5 | PRMT5-IN-27 (compound 481) is an inhibitor (blocker/antagonist) of PRMT5. |
|
V51599 | PRMT5-IN-28 | 2242753-66-6 | PRMT5-IN-28 (compound 36) is a coupling agent for the protein arginine methyltransferase 5 (PRMT5) enzyme. |
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