|
T17204 |
UNC0321
|
|
Histone Methyltransferase
|
|
UNC0321 is an effective inhibitor of histone methyltransferase G9a with a Ki of 63 pM and with IC50s 9 nM and 6 nM in ECSD and CLOT assays. UNC0321 inhibits GLP with IC50s of 15 nM and 23 nM in ECSD and CLOT assays. |
|
T7378 |
BRD9539
|
|
Histone Methyltransferase
|
|
BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2), also known as G9a, with an IC50 value of 6.3 μM |
|
T1923 |
BRD4770
|
|
Histone Methyltransferase
|
|
BRD4770 is a histone methyltransferase G9a inhibitor and induces cell senescence. |
|
T2354 |
UNC 0631
|
UNC0631 |
Histone Methyltransferase
|
|
UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM). |
|
T17203 |
UNC0224
|
|
Histone Methyltransferase
|
|
UNC0224 is a selective inhibitor of G9a with a Ki of 2.6 nM and IC50 of 15 nM. UNC0224 also potently inhibits GLP with assay-dependent IC50 values of 20-58 nM. |
|
TQ0232 |
UNC0646
|
UNC 0646 |
Histone Methyltransferase
|
|
UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50s: 6 nM/15 nM for G9a/GLP). UNC0646(UNC 0646) potently blocks G9a/GLP methyltransferase activity in cells ... |
|
T7194 |
CM-272
|
|
Apoptosis
,
DNA Methyltransferase
,
Histone Methyltransferase
|
|
CM-272 is a dual G9a/DNA methyltransferases (DNMTs) inhibitor. |
|
T4166 |
UNC0642
|
UNC-0642,UNC 0642 |
Histone Methyltransferase
|
|
UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM). |
|
T1959 |
BIX-01294 trihydrochloride
|
BIX 01294 |
Histone Methyltransferase
,
Autophagy
|
|
BIX-01294 trihydrochloride is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase. |
|
T7697 |
BIX-01294
|
|
Histone Methyltransferase
,
Autophagy
|
|
BIX-01294 is an G9a Histone Methyltransferase inhibitor(IC50 : 1.9 μM). |
|
T28112 |
MS0124
|
MS 0124,MS-0124 |
Histone Methyltransferase
|
|
MS0124 is a potent and selective G9A-like protein (GLP) inhibitor with IC50 values of 13±4 nM and 440±63 nM, respectively. |
|
T10882 |
CPUY074020
|
|
Histone Methyltransferase
|
|
CPUY074020 is a potent and orally bioavailable inhibitor of histone methyltransferase G9a (IC50: 2.18 μM) with anti-proliferative activity. |
|
T3624 |
A-366
|
A 366,A366 |
Epigenetic Reader Domain
,
Histone Methyltransferase
|
|
A-366 is a highly selective peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP, respectively.It is more than 1,000-fold selective for G9a and GLP over the other 21 met... |
|
T10840L |
CM-579
|
|
DNA Methyltransferase
,
Histone Methyltransferase
|
|
CM-579 is a dual inhibitor of G9a and DNMT( IC50:16 nM, 32 nM for G9a and DNMT). It has potent in vitro cellular activity in a wide range of cancer cells. |
|
T3257 |
UNC0638
|
|
Influenza Virus
,
Histone Methyltransferase
,
Autophagy
|
|
UNC0638 is an inhibitor of β-protein lysine methyltransferases G9a(IC50<15 nM) and GLP(IC50=19 nM) with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets. |
|
T63140 |
LSD1-IN-20
|
|
Histone Demethylase
|
|
Lsd1-in-20 is a potent dual inhibitor of LSD1/G9a with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 showed antiproliferative activity against THP-1 leukemia cells and MDA-MB-231 breast cancer cells in vitro, w... |
|
T63351L |
MS8511 HCl
|
MS8511 HCl(2866408-21-9 Free base) |
Histone Methyltransferase
|
|
MS8511 HCl is a selective and potent covalent inhibitor of G9a/GLP that acts by targeting cysteine residues in the substrate binding site. MS8511 has anticancer activity and antiproliferative activity and reduces intrace... |
|
T67947 |
WDR5-0102
|
|
Histone Methyltransferase
|
|
WDR5-0102 is a compound that inhibits the WDR5-MLL1 interface (K dis = 7 μM, K d = 4 μM), selectively reducing MLL1 HMT activity without affecting the human H3K4 methyltransferase SETD7 or other HMTs, including G9a, EHMT... |
|
T11185 |
EML741
|
|
Histone Methyltransferase
|
|
EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated. EML741 is a histone lysine methyltransferase... |
|
T79249 |
Antitumor agent-101
|
|
Histone Methyltransferase
|
|
Antitumor agent-101 is a selective, covalent inhibitor targeting lysine methyltransferases G9a/GLP, demonstrating IC50 values of 8.5 nM for G9a and 5.5 nM for GLP. It exhibits antitumor efficacy in the PANC-1 xenograft m... |
|
T79776 |
ZZM-1220
|
|
Histone Methyltransferase
|
|
ZZM-1220, a covalent inhibitor of histone lysine methyltransferase G9a/GLP, exhibits IC50 values of 458 nM for G9a and 924 nM for GLP. It effectively inhibits H3K9me2 in cells, induces apoptosis in triple-negative breast... |
|
T71824 |
CSV0C018875 Hydrochloride
|
|
|
|
CSV0C018875 Hydrochloride is a novel G9a (EHMT2) inhibitor, binding tightly inside the active site cavity of G9a, inhibiting the activity of G9a in both enzyme and cell based assays with much lesser toxicity than BIX-012... |
|
T27132 |
DCG066
|
|
|
|
DCG066 is a G9a inhibitor in vitro. |
|
T10840 |
CM-579 trihydrochloride (1846570-40-8 free base)
|
CM-579 trihydrochloride |
DNA Methyltransferase
|
|
CM-579 trihydrochloride is a first-in-class reversible and dual inhibitor of G9a and DNMT (IC50s: 16 nM, 32 nM) with potent in vitro cellular activity in a wide range of cancer cells. |
|
T28111 |
MS012
|
MS-012,MS 012 |
|
|
MS012 is a Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase (Kd = 46 ± 15 nM). |
|
T26188 |
Setin-1
|
|
|
|
Setin-1 is the most potent Set7 inhibitor that acts by inhibiting the KMTase G9a. |
|
T73188 |
RK-0133114
|
|
|
|
RK-0133114, a G9a inhibitor and the R-enantiomer of RK-701, exhibits potent inhibition of G9a with an IC50 value of 3.7 μM. This compound is utilized in research focused on sickle cell disease (SCD) [1]. |
|
T60786 |
CSV0C018875
|
|
|
|
CSV0C018875 is a quinoline-based EHMT2/G9a inhibitor with lower cytotoxicity than BIX-01294 [1]. |
|
T72277 |
CM-579 trihydrochloride
|
|
|
|
CM-579 trihydrochloride, a first-in-class reversible, dual inhibitor of G9a and DNMT, exhibits potent in vitro cellular activity across a broad spectrum of cancer cells. It demonstrates inhibition with IC50 values of 16 ... |
|
T63351 |
MS8511
|
|
|
|
MS8511, a selective covalent irreversible inhibitor of G9a/GLP, targets a cysteine residue at the substrate binding site, displaying IC50 values of 100 nM (G9a) and 140 nM (GLP), alongside Kd values of 44 nM (G9a) and 46... |
|
T35567 |
BIX01294 (hydrochloride hydrate)
|
|
|
|
The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3)... |
|
T22250 |
5WKS
|
ZINC97756584 |
Others
|
|
5WKS also known as ZINC97756584 is a biochemical. It is a G9a protein inhibitor.G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes H3K9me2, a reversible modification commonly associated with transcrip... |
|
T73517 |
RK-701
|
|
|
|
RK-701, a highly selective and non-genotoxic G9a inhibitor, exhibits an IC 50 value of 23-27 nM. It selectively up-regulates HbF, γ-Globin, and BGLT3 expression while down-regulating H3K9me2 expression. Additionally, RK-... |
|
T38784 |
Histone H3 (1-25), amide
|
Histone H3 (1-25), amide |
|
|
Histone H3 (1-25), amide is a N-terminal peptide fragment of histone H3 that serves as a substrate for histone methyltransferases (HMTs). It can be utilized to identify the substrate for HMTs. Compared to histone H3 (15-... |
