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 |
|---|---|---|---|---|
|
V0380 | GSK343 | 1346704-33-3 | GSK343 is a novel, highly potent and selective inhibitor of H3-lysine 27 (H3K27) methyltransferase EZH2with antineoplastic activity. |
|
V0387 | GSK503 | 1346572-63-1 | GSK503 (GSK-503) is a novel, potent and specific inhibitor of Enhancer of zeste homolog 2 (EZH2)methyltransferase inhibitor with potential antitumor activity. |
|
V80243 | HDAC3-IN-2 | HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50= 14 nM) that efficiently targets triple-negative breast cancer cells. | |
|
V2821 | HLCL-61(HCl) | 1158279-20-9 | HLCL-61 hydrochloride is a potent, selective, first-in-class small-molecule inhibitor of PRMT5 (protein arginine methyltransferase) that has the potential for treatment of acute myeloid leukemia. |
|
V56081 | Igermetostat | 2409538-60-7 | Igermetostat is an EZH2 inhibitor used in in vivo and in vitro cancer research. |
|
V78106 | IHMT-EZH2-426 | IHMT-EZH2-426 (compound 38) is a potent covalent EZH2 degrader with IC50 of 1.3 nM, 1.2 nM and 1.7-3.5 nM against EZH2 wild type, EZH2-A687V and EZH2-Y641F/Y641N/Y641S, respectively. | |
|
V79149 | iPRMT1 | iPRMT1 is a potent and specific PRMT1 inhibitor that may be utilized in breast cancer research. | |
|
V3136 | JQ-EZ-05 (JQEZ5) | 1913252-04-6 | JQ-EZ-05 (also abbreviated as JQEZ5) is a novel, potent, specific and reversible inhibitor of EZH2 (overexpressed in tumor cells such as lung cancer). |
|
V80555 | LEM-14-1189 | LEM-14-1189, a LEM-14 analogue, is an NSD inhibitor (antagonist) with IC50s of 418 μM (NSD1), 111 μM (NSD2), and 60 μM (NSD3). | |
|
V2607 | Lirametostat (CPI-1205) | 1621862-70-1 | Lirametostat (CPI-1205; CPI 1205, CPI1205)is an orally bioavailable and selective inhibitor of EZH2 (enhancer of zeste homologue 2, a histone lysine methyltransferase) with potential antitumor activity. |
|
V3138 | LLY-283 | 2040291-27-6 | LLY-283 (LLY283) is the first-in-class and selective SAM-competitive inhibitor of PRMT5 (protein arginine methyltransferase 5) with antitumor activity. |
|
V24271 | LLY-507 | 1793053-37-8 | LLY-507 (LLY507) is a novel, potent, cell-permeable/active and selective inhibitor ofprotein-lysine methyltransferase SMYD2 (SET And MYND Domain Containing 2) with potential anticancer activity. |
|
V24932 | MAK-683 | 1951408-58-4 | MAK-683 (MAK683; extracted from patent US20160176882 A1, compound example 2) is a novel and potent embryonic ectoderm development protein (EED) inhibitor and allosteric inhibitor of polycomb repressive complex 2 (PRC2) with potential anticancer activity. |
|
V76797 | MAK683-CH2CH2COOH hydrochloride | MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein). | |
|
V0398 | MI-3 | 1271738-59-0 | MI-3 (Menin-MLL Inhibitor 3) is a novel and potent inhibitor of menin-MLL interaction with potential antitumor activity. |
|
V25509 | MI-503 | 1857417-13-0 | MI-503 (MI503) is a novel,orally bioavailable and potent Menin-MLL interaction inhibitor(IC50= 14.7 nM) with potential anticancer activity. |
|
V0400 | MM-102 | 1417329-24-8 | MM-102 (also known as HMTase Inhibitor IX) is a novel and potent peptidomimetic inhibitor of MLL1 (Mixed lineage leukemia 1) with anticancer activity. |
|
V32086 | MM-102 TFA | 1883545-52-5 | MM-102 TFA (the trifluoroacetic acid salt of MM-102) is a novel, potent,high-affinity peptidomimeticMLL1inhibitor withIC50of 0.4 μM in a cell-free assay. |
|
V22884 | MM-401 | 1442106-10-6 | MM-401 is a novel, potent and selective inhibitor of histone H3K4 methyltransferase MLL1 activity. |
|
V41182 | MM-589 TFA | 2253167-09-6 | MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interactions. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
