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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V3454 | BIX01338 | 1228184-65-3 | BIX-01338 is a novel and potenthistone lysine methyltransferaseG9a inhibitor with an IC50 value of 4.7µM. |
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V55740 | BML-278 | 120533-76-8 | BML-278 is a SIRT1 activator (EC150: 1 μM). |
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V51601 | BRD-0639 | 2760881-74-9 | BRD0639 is a transcriptional inhibitor of the PRMT5-substrate adapter interaction. |
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V0394 | BRD4770 | 1374601-40-7 | BRD4770 (BRD-4770) is a novel and selective inhibitor ofG9a (ahistone methyltransferase, also known as euchromatin histone methyltransferase 2 (EHMT2))with anticancer activity. |
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V3455 | BRD9539 | 1374601-41-8 | BRD9539 is a potent and selective inhibitor that inhibits G9a activity with an IC50 of 6.3 μM, it also inhibits euchromatin histone methyltransferase 2 (EHMT2). |
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V2926 | C-7280948 | 587850-67-7 | C-7280948 (C7280948) is a selective PRMT1 (protein arginine methyltransferase) inhibitor with anticancer activity. |
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V56086 | C21 | 1229236-78-5 | C21 is a potent, irreversible, and selective inhibitor of PRMT1 with IC50 of 1.8 μM. |
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V78642 | CARM1 degrader-1 | CARM1 degrader-1 (compound 3b) is a degrader (DC50=8.1 nM) of co-activator associated argininemethyltransferase (CARM1). | |
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V78643 | CARM1 degrader-2 | CARM1 degrader-2 (compound 3e) is a degrader (DC50=8.8 nM) of co-activator associated argininemethyltransferase (CARM1). | |
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V56089 | CARM1-IN-3 | 912970-67-3 | CARM1-IN-3 (compound 17b) is a potent and specific inhibitor of co-activator associated argininemethyltransferase (CARM1) with IC50 of 0.07 µM. |
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V3456 | Chaetocin | 28097-03-2 | Chaetocin, a naturally occurring fungal mycotoxin extracted from Chaetomium, is a novel and non-specific inhibitor of the histone lysine methyltransferase (HMT) G9a with anIC50of 2.5 μM. |
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V79014 | cis-BG47 | cis-BG47 is the cis isomer of BG47, a typical histone deacetylase HDAC1 or HDAC2 selective photoepigenetic probe that can induce trans-cis isomerization during light Binds to HDAC target and competitively inhibits its deacetylase activity, increasing acetylation of Histone Methyltransferase H3K9. | |
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V3105 | CM-272 | 1846570-31-7 | CM-272 (CM272) is a first-in-class, reversible, and dual inhibitor of G9a and DNMTs in hematological malignancies with antineoplastic effects. |
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V77145 | CM-579 trihydrochloride | CM-579 tri HCl is a first-in-class, reversible, dual (bifunctional) inhibitor of G9a and DNA methyltransferase (DNMT), with IC50s of 16 nM and 32 nM respectively. | |
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V39060 | CMP-5 | 880813-42-3 | CMP-5(PRMT5-IN-5) is a first-in-class and specific PRMT5 inhibitor with anticancer (B-cell lymphomas) and immunomodulatory activity. |
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V56079 | CPI-1328 | 2390367-27-6 | CPI-1328 is an EZH2 inhibitor (antagonist) with Ki of 63 fM. |
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V0389 | CPI-169 | 1450655-76-1 | CPI-169 (CPI169) is a novel, potent, and selective inhibitor of EZH2 (enhancer of zeste homolog 2) inhibitor with anticancer activity. |
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V0386 | CPI-360 | 1802175-06-9 | CPI-360 is a novel, highly potent, selective, and SAM-competitive inhibitor of enhancer of zeste homolog 2 (EZH2) with potential antitumor activity. |
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V52216 | CSV0C018875 | 442150-41-6 | CSV0C018875 is a quinoline-based inhibitor of EHMT2/G9a. |
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V19289 | DCLX069 | 792946-69-1 | DCLX069 (DCLX-069) is a novel,SAM-competitive and selective PRMT1 (protein arginine methyltransferase 1) inhibitor (IC50 =17.9 µM) with anticancer effects. |
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