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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)

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Cat. No. Product Name Information
PC-25505

KCC-07

MBD2 inhibitor

KCC-07 is a potent, selective and BBB-penetrable inhibitor of MBD2 (methyl CpG binding domain protein 2), prevents binding of MBD2 to methylated DNA, reactivates ADGRB1 expression and prevents MDM2-mediated p53 polyubiquitination.
PC-25447

DNMT2 inhibitor 16

DNMT2 inhibitor

DNMT2 inhibitor 16 is a potent, selective DNMT2 (TRDMT1) inhibitor with ITC KD of 3.04 uM, reduces m5C levels in MOLM-13 tRNA and synergizes with doxorubicin to impair cell viability, targeting a cryptic allosteric binding site.
PC-25322

IACS-17817

NSD2 inhibitor

IACS-17817 is a highly potent, selective and SAM-competitive inhibitor of NSD2 (MMSET, WHSC1) with IC50 of 19.0 nM, >50-fold selective over a KMT panel including NSD1, NSD3 and SETD2.
IACS-17817 inhibits NSD2 methylation of nucleosome substrates in vitro with IC50 of 19.0 nM.
PC-25273

UNC0646

G9a inhibitor

UNC0646 (UNC 0646) is a potent, selective and cell-active inhibitor of G9a methyltransferase with IC50 of 6 nM in SAHH-coupled assays, reduces H3K9me2 levels in MDA-MB-231 cells with IC50 of 26 nM.
PC-25272

UNC0631

G9a inhibitor

UNC0631 (UNC 0631) is a potent, selective and cell-active inhibitor of G9a methyltransferase with IC50 of 4 nM in SAHH-coupled assays, reduces H3K9me2 levels in MDA-MB-231 cells with IC50 of 25 nM.
PC-24896

KMT9 inhibitor 7b

KMT9 inhibitor

KMT9 inhibitor 7b is a potent and selective lysine methyltransferase 9 (KMT9) inhibitor with Kd of 10 nM.
PC-24895

KMT9 inhibitor 8

KMT9 inhibitor

KMT9 inhibitor 8 is the ethyl ester prodrug of KMT9 inhibitor 7b, a potent and selective lysine methyltransferase 9 (KMT9) inhibitor with Kd of 10 nM.
PC-24527

HH2853

EZH1/2 inhibitor

HH2853 is a novel potent dual EZH1/2 inhibitor that effectively inhibit the catalytic activity of wild-type EZH2 and mutated forms (A677G, Y641F, Y641N, and Y641C) with IC50 of 3.75, 2.21, 2.65, and 2.62 nM respectively, synchronously suppresses EZH1 activity with IC50 of 9.26 nM.
PC-24375

CM112

PRMT1 degrader

CM112 is a potent, selective PRMT1 degrader designed by tethering adamantane to MS023 via a 5-PEG linker, has DC50 of 0.83 uM in MCF-7 cells.
PC-24337

iZMYND8-34

ZMYND8 inhibitor

iZMYND8-34 is a small molecule inhibitor of histone reader zinc finger MYND-type containing 8 (ZMYND8), inhibits ZMYND8 histone recognition, effectively blocks neuroendocrine prostate cancer (NEPC) development.
PC-24292

Dual CARM1-IKZF3 inhibitor 074

CARM1/IKZF3 inhibitor

Dual CARM1-IKZF3 inhibitor 074 is a compound composed of the CARM1 inhibitor EZM2302, linked to pomalidomide, increases CRBN-dependent IKZF1, IKZF3, ZFP91, and FGD3 protein degradation, inhibits CRAM1 with IC50 of 2 nM.
PC-24113

Balomenib

Menin-KMT2A inhibitor

Balomenib (Balamenib, ZE63-0302) is an oral small molecule inhibitor of the menin-KMT2A interaction.

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