Histone Methyltransferase (HMTase)

31 products · Page 1 of 1

All small molecule research tools

DC7332

UNC-1215

UNC1215 is a potent and selective chemical probe for the methyllysine (Kme) reading function of L3MBTL3 with Kd value of 120 nM.

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DC7331

UNC-0638

UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC50s of less than 15 nM and 19 nM, respectively.

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DC7374

BIX01294

BIX-01294 is an inhibitor of G9a Histone Methyltransferase with IC50 of 1.9 μM.

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DC8537

AZ505

AZ505 is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.

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DC7915

UNC0321

UNC0321 is a potent and selective G9a inhibitor with Ki of 63 pM, UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date.It was found that replacing the 5-carbon chain in…

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DC7671

UNC0379

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.UNC0379 is a synthetic small-molecule inhibitor that…

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DC7927

EPZ011989

EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.IC50 value: < 3 nM ( Ki for wt…

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DC8544

MI-463

MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.

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DC8044

GSK503

GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Kiapp values of 3 to 27 nM.

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DC7674

BRD4770

BRD4770 is a novel G9a(EHMT2) inhibitor with EC50 of 5 uM (trimethylated H3K9 in PANC-1 cell).

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DC7855

A-366

A-366 is a potent histone methyltransferase G9a inhibitor with an IC50 of 3.3 nM.

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DC7679

(R)PFI-2 HCl

PFI-2 hydrochloride is a a first-in-class, potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 with IC50 of 2 nM, 500 fold active than (S)-PFI-2.(R)-PFI-2 is highly selective…

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DC8061

SGC-707

SGC707 is a first-in-class PRMT3 chemical probe which is a potent, selective, and cell-active allosteric inhibitor of PRMT3 with IC50 of 31 nM.

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DC8012

EPZ015666

EPZ015666 is an orally available inhibitor of PRMT5 with an IC50 of 22 nM.

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DC9267

EPZ015866

EPZ015866 is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 22 nM.

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DC10647

EPZ015938(pemrametostat)

GSK3326595 is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC50 of 6.2 nM.

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DC7562

MM-102

MM-102 is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.

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Structure information available on request

DC7856

LLY-507

LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2 with an IC50 of 15 nM.

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DC10509

A-196

A-196 is a potent and selective chemical inhibitor of SUV420H1 and SUV420H2 that inhibits the di- and trimethylation of H4K20me in multiple cell lines. Target: A-196 is a selective chemical probe for SUV420H1/H2. A-196…

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DC9965

UNC3866

UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen (IC50=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel.

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Structure information available on request

DC4242

Pinometostat(EPZ5676)

Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.

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DC7143

GSK-343

GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.

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DC9985

OICR9429

OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction with IC50 of 5 uM. inhibit proliferation and induce differentiation

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DC47616

EPZ-719

EPZ-719 is a novel and potent SETD2 inhibitor ( IC50 = 0.005 μM) with a high selectivity over other histone methyltransferases.

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DC72540

MS8815

MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC50 value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC).

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DC70785

SKLB-03176

SKLB-03176 (SKLB03176) is a potent, selective, covalent EZH2 inhibitor with IC50 of 47 nM, covalently binds to the SAM pocket of EZH2.SKLB-03176 showed good inhibitory activity against mutations EZH2 Y641F, EZH2 Y641N,…

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DC9678

HLCL-61 hydrochloride

HLCL-61 hydrochloride is a first-in-class small-molecule inhibitor of PRMT5. Target: PRMT5in vitro: HLCL-61 shows effective inhibition of symmetric arginine dimethylation (me2) of histones H3 and H4 in AML samples,…

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DC10885

BCI-121

BCI-121 significantly inhibits SMYD3-substrate interaction and chromatin recruitment and is effective in reducing proliferation in various cancer cells types. BCI-121 significantly reduces proliferation of HT29 (by…

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DC70095

NSD1 inhibitor BT5

1. Huang H, et al. Nat Chem Biol. 2020 Dec;16(12):1403-1410. Chemical & Physical Properties

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DC73322

DP308

DP308 is a novel and effective 53BP1 tandem Tudor domain (TTD) inhibitor, disrupts the binding between 53BP1 and H4K20me2 peptide with IC50 of 1.69 uM.

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DC9293

MS023

MS023 is a potent, selective, and cell-active inhibitor of human type I PRMTs with IC50 of 4-119 nM.

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