Histone Methyltransferase (HMTase)

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Cat. No.	Product Name	Field of Application
DC9678	HLCL-61 hydrochloride Featured	HLCL-61 is a first-in-class small-molecule inhibitor of PRMT5 for treatment of acute myeloid leukemia.
DC11421	JQEZ5 Featured	JQEZ5 is a novel and potent EZH2 inhibitor.
DC7856	LLY-507 Featured	LLY-507 is a chemical probe for SMYD2 (a protein lysine methyltransferase).
DC10560	MAK683 Featured	MAK683 is a novel PRC2/EED inhibitor.
DC8546	MI-136 Featured	MI-136 inhibits DHT-induced expression of androgen receptor (AR) target genes.
DC8544	MI-463 Featured	MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
DC8545	MI-503 Featured	MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-MLL interaction.
DC10287	MI-538 Featured	MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM.
DC7562	MM-102 Featured	MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.
DC9293	MS023 Featured	MS023 is a potent, selective, and cell-active inhibitor of human type I PRMTs with IC50 of 4-119 nM.
DC8805	MS049 (hydrochloride) Featured	MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 that is active in cells.
DC8823	XY1 Featured	Negative control of SGC 707. Exhibits >3000-fold lower potency (IC50 >100 μM) compared to the active analog.
DC9985	OICR9429 Featured	OICR-9429 is a potent and selective chemical probe suitable to help dissect the biological role of WDR5 (Kdisp < 100 nM).
DC11257	OTS186935 Featured	OTS186935 (OTS-186935) is a potent, in vivo-active inhibitor of protein methyltransferase SUV39H2 with IC50 of 6.49 nM, inhibits A549 cell growth with IC50 of 0.67 uM; causes a significant growth inhibitory effect in mouse xenograft models using MDA-MB-231 breast cancer cells as well as A549 lung cancer cells, at 25 mg/kg once daily for 14 days yielded a TGI of 60.8%; attenuates the levels of H3K9me3 in A549 xenograft mouse model.
DC11256	OTS193320 Featured	OTS193320 (OTS-193320) is a potent inhibitor of protein methyltransferase SUV39H2 with IC50 of 22.2 nM.
DC10634	PF-06726304	PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM.
DC11153	PF-06855800	PF-06855800 (PF06855800) is a potent, selective, SAM competitive, BBB-penetrant, orally active inhibitor of protein arginine methyltransferase PRMT5 with Ki of 0.02 nM.
DC7679	(R)PFI-2 HCl Featured	PFI-2 is a novel potent and selective SETD7 histone lysine methyltransferase inhibitor with IC50 ~2 nM. It has > 100-fold selectivity over other methyltransferases and other non-epigenetic targets.
DC8061	SGC-707 Featured	SGC 707 is a potent allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) (IC50 = 31 nM).
DC10429	SGC2085 Featured	SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 50 nM.
DC11226	T1551	T1551 is a novel selective PRMT5 inhibitor with IC50 of 34.1 uM, decreases cell viability of A549 cell with IC50 of 5.8 uM (72h).
DC8293	UNC-0224 Featured	UNC-0224 is a potent inhibitor of G9a histone lysine methyltransferase (IC50 = 15 nM).
DC7915	UNC0321 Featured	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.IC50 value: 63 pM(Ki); 9 nM (ECSD assay) [1]Target: G9aIt was found that replacing the 5-
DC7671	UNC0379 Featured	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.
DC7331	UNC-0638 Featured	UNC0638 is an inhibitor of 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.
DC10024	UNC-1079 Featured	UNC1079 is the piperidine analog of UNC1021, as a structurally similar but significantly less potent inhibitor for use as a negative control in cellular studies.
DC7332	UNC-1215 Featured	UNC1215 is a potent and selective chemical probe for the methyllysine (Kme) reading function of L3MBTL3 with Kd value of 120 nM.
DC9965	UNC3866 Featured	UNC3866 is a potent and selective antagonist of CBX4 and CBX7 chromodomains with (Kd ≈ 100 nM). It is 6- to 63-fold selective for these chromodomains over the other CBX and CDY chromodomains.
DC8662	WDR5-0103 Featured	WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM.
DC28333	BI-9321	BI-9321 is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells.

Histone Methyltransferase (HMTase)

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