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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-25825

I3IN-002

IGF2BP3 inhibitor

I3IN-002 is a small molecule inhibitor of RNA-binding protein IGF2BP3, inhibits IGF2BP3-RNA interactions and shows leukemic cell growth-inhibitory activity with IC50 of ~2 µM in wild-type SEM-cells.
PC-25711

Heterochromatin protein 1 inhibitor (R)-18

HP1 inhibitor

Heterochromatin protein 1 inhibitor (R)-18 is a small-molecule inhibitor of heterochromatin protein 1 (HP1), inhibits the HP1/H3K9me3 interaction with IC50 of 18.1 uM.
PC-25566

BMF-219

Menin inhibitor

BMF-219 (Icovamenib) is a potent, selective and covalent irreversible menin inhibitor, inhibits the growth of KRAS-mutated solid tumors with G12C, G12D, and G12V KRAS mutations.
PC-25565

RK-552

NSD2 inhibitor

RK-0080552 (RK-552) is a potent, specific small molecule NSD2 inhibitor with IC50 of 0.11 uM, weakly inhibits G9a (IC50=1.2 uM) and does not inhibit SET7/9.
PC-25506

LH168

WDR5 inhibitor

LH168 is a potent, exquisitely selective WDR5 chemical probe inhibitor with EC50 of 10 nM in cellulo target engagement NanoBRET assays, SPR KD of 1.9 nM.
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-25006

SHR2554

EZH2 inhibitor

Zeprumetostat (SHR2554) is a potent, highly selective EZH2 inhibitor, specifically inhibits both wild-type (IC50=0.87 nM) and mutant (EZH2(Y641F), IC50=2.68 nM) EZH2 methyltransferase activity with similar potencies.
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.

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