EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
A-366 is a potent histone methyltransferase G9a inhibitor with an IC50 of 3.3 nM.
BCI-121 is a SMYD3 inhibitor that impairs the proliferation of cancer cell.
DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity[1].
UNC0379 trifluoroacetate is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8 with IC50 of 7.3±1.0 uM; selective over 15 other methyltransferases.IC50 value: 7.3±1.0 uMTarget: SETD8 inhibitorUNC0379 is a synthetic small-molecule inhibitor that displays inhibitory activity in multiple biochemical assays and is selective for SETD8 over 15 other methyltransferases. The binding affinity of UNC0379 to SETD8 was determined using biophysical assays such as ITC (isothermal titration calorimetry) and SPR (surface plasmon resonance) and is largely consistent with its potency in biochemical assays.
WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines[1].
PRMT5-IN-14 is a PRMT5 inhibitor to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8 with IC50 of 7.3±1.0 uM; selective over 15 other methyltransferases.IC50 value: 7.3±1.0 uMTarget: SETD8 inhibitorUNC0379 is a synthetic small-molecule inhibitor that displays inhibitory activity in multiple biochemical assays and is selective for SETD8 over 15 other methyltransferases. The binding affinity of UNC0379 to SETD8 was determined using biophysical assays such as ITC (isothermal titration calorimetry) and SPR (surface plasmon resonance) and is largely consistent with its potency in biochemical assays.
CM-272 (CM272) is a novel potent, selective and reversible dual inhibitor of G9a/DNMTs with IC50 of 8 nM and 382 nM for G9a and DNMT1, respectively; also inhibits DNMT3A/3B/GLP with IC50 of 85/1,200/2 nM, respectively; inhibits cell proliferation and promotes apoptosis in different haematological neoplasias (AML, ALL and DLBCL); significantly prolongs survival of AML, ALL and DLBCL xenogeneic models.
MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
MR837 is an inhibitor of NSD2-PWWP1. MR837 can bind with human nuclear receptor binding SET domain protein 2 (PWWP domain)[1].
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.
EZH2-IN-2 is a EZH2 inhibitor extracted from patent WO2018133795A1, Compound Example 69, with an IC50 of 64 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity[1].