Histone Methyltransferase

Histone methyltransferases (HMT) are histone-modifying enzymes , that catalyze the transfer of one, two, or three methyl groups to lysine and arginine residues of histone proteins. The attachment of methyl groups occurs predominantly at specific lysine or arginine residues on histones H3 and H4.

カタログ番号	製品名
T12939	SMYD2-IN-1	SMYD2-IN-1 is an inhibitor of SMYD2 (IC50 of 4.45 nM).
T11436	GNA002	GNA002 is a highly potent, specific, and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor (IC50: 1.1 μM).
T22325	EPZ020411 hydrochloride	EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.
T11084	Dot1L-IN-5	Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein ( DOT1L ) inhibitor with an IC 50 SPA DOT1L of 0.17 nM [1].
TN5097	Tanshindiol C	Tanshindiol C protects macrophages from oxLDL induced foam cell formation via activation of Prdx1/ABCA1 signaling and that Prdx1 may be a novel target for therap...
T1987	PFI-2	PFI-2 is an effective, specific and cell-active lysine methyltransferase SETD7 inhibitor (Ki/IC50: 0.33/2 nM), 1000-fold selectivity over other methyltransferase...
T10427	AZ505 ditrifluoroacetate	AZ505 ditrifluoroacetate is an effective and selective SMYD2 inhibitor (IC50: 0.12 μM).
T27133	DCLX069	DCLX069 is a potent and selective PRMT1 inhibitor. DCLX069 occupies the SAM binding pocket to exert the inhibitory effect. DCLX069 effectively blocks cell prolif...
T11185	EML741	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 barri...
T11082	Dot1L-IN-2	Dot1l-in-2 is an effective, selective and oral bioutilization inhibitor of histone methyltransferase Dot1L, with IC50 and Ki of 0.4 nM and 0.08 nM, respectively....
T10882	CPUY074020	CPUY074020 is a potent and orally bioavailable inhibitor of histone methyltransferase G9a (IC50: 2.18 μM) with anti-proliferative activity.
T4334	EPZ020411 2HCl (1700663-41-7(free base))	EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).
T22342	GSK3368715 3HCl	GSK3368715, a potent inhibitor of type I protein arginine methyltransferases (PRMT), could inhibit PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 ...
T13279	Valemetostat tosylate	Valemetostat tosylate is a dual inhibitor of EZH1/2 and used in the research of relapsed/refractory peripheral T-cell lymphoma.
T6292	3-Deazaneplanocin A	3-Deazaneplanocin A (DZNep) is an attractive epigenetic anticancer agent through the inhibition of the cellular enhancer of zeste homolog 2 (EZH2) protein.
T11500	GSK3368715	GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: ...
T2354	UNC 0631	UNC0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).
TN5096	Tanshindiol B	Tanshindiol B possesses a unique anti-cancer activity whose mechanism involves the inhibition of EZH2 activity and would provide chemically valuable information ...
T11500L	GSK3368715 dihydrochloride	GSK3368715 dihydrochloride is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) in...
T12541	PRMT5-IN-1	PRMT5-IN-1 is a covalent inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50 of 11 nM for PRMT5/MEP50).
T12428	PF-06726304 acetate	PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity.
T16577	PRMT5-IN-2	PRMT5-IN-2 is an inhibitor of protein arginine methyltransferase 5.
T15240	Tazemetostat trihydrochloride	Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing ...
T9700	EZH2-IN-2	EZH2-IN-2 is a EZH2 inhibitor with an IC50 of 64 nM (Patent WO2018133795A1, Compound Example 69).
T3081L	EPZ004777 hydrochloride	EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
T6810	CPI-360	CPI-360 is a potent, selective, and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
T11083	Dot1L-IN-4	Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM.
T12940	SMYD3-IN-1	SMYD3-IN-1 is an irreversible and selective SMYD3 (SET and MYND domain containing 3) inhibitor(IC50 of 11.7 nM).
T11081	Dot1L-IN-1	The Ki value of DOT1L-in-1 is 2pm.It is a highly effective, selective and novel Dot1L inhibitor.
T6360	3-deazaneplanocin A HCl	3-deazaneplanocin A (DZNeP)HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM.
T13954	UNC6852	UNC6852 contains an EED ligand (IC50 = 247 nM) and a von Hippel-Lindau ligand and is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC.
T10840L	CM-579	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.
T6803	Chaetocin	Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a an...
T40254	MRTX-1719	MRTX-1719 is a potent, first-in-class, selective inhibitor of the PRMT5/MTA complex, with an IC50 of less than 10 nM in PRMT5/MTA MTAP DEL SDMA cells.
T9584	UNC6934	UNC6934 is a chemical probe targeting the N-terminal PWWP (PWWP1) domain of NSD2.
T28036	MI-2-2	MI-2-2 is an inhibitor of bivalent protein-protein interaction between menin and MLL with an IC50 of 46 nM. MI-2-2 binds to menin with Kd of 22 nM.
T2643	MI-3	MI-3 (Menin-MLL Inhibitor) is an effective inhibitor of Menin-MLL interaction (IC50: 648 nM).
T29231	ZLD1039	ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic acti...
T9742	SETDB1-TTD-IN-1	SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive inhibitor of SETDB1-TTD with a Kd of 88 nM.
T9969	EZM0414	EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 ( IC 50 =18 nM in SETD2 biochemical assay; IC 50 =34 nM in cellular assay). EZM0414 can be...
T10205	A-395	A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12, IC5...
T60002	Ethyl 2-amino-4-methyl-5-[(3-nitrophenyl)carbamoyl]thiophene-3-carboxylate	Ethyl 2-amino-4-methyl-5-[(3-nitrophenyl)carbamoyl]thiophene-3-carboxylate is a selective inhibitor of histone methyltransferase SETD7 (IC50 = 4.59 μM) with anti...
T10682L	CARM1-IN-1	CARM1-IN-1 is a selective inhibitor of CARM1 with IC50 of 8.6 μM. CARM1-IN-1 shows weak activity against PRMT1 and SET7 with IC50 > 600 μM.
T7305	JQEZ5	JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM).
T9399	Menin-MLL inhibitor 20	Menin-MLL inhibitor 20 is an irreversible inhibitor of menin-MLL interaction with antitumor activities (WO2020142557A1, compound 6).
T5484	GSK467	GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).
TQ0232	UNC0646	UNC 0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50s: 6 nM/15 nM for G9a/GLP). UNC0646 potently b...
T0174	Cyproheptadine hydrochloride sesquihydrate	Cyproheptadine hydrochloride sesquihydrate, an antihistamine, is an antagonist of serotonin and histamine2.
T21826	TC-E 5003	TC-E 5003 is a selective inhibitor of PRMT1 with IC50 of 1.5 μM.
T5745	GSK3326595	GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).