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.

Cat No.	product name
T0174	Cyproheptadine hydrochloride	Cyproheptadine hydrochloride sesquihydrate, an antihistamine, is an antagonist of serotonin and histamine2.
T1775	GSK503	GSK-503, a potent EZH2 inhibitor, has potential antitumor activity.
T1788	EPZ6438	Tazemetostat is an orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyltransferase EZH2, with pote...
T1841	UNC0379	UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8.
T1868	JIB-04	JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.
T1905	EPZ005687	EPZ005687 is a potent and selective inhibitor of EZH2.
T1923	BRD4770	BRD4770 is a histone methyltransferase G9a inhibitor and induces cell senescence.
T1959	BIX 01294 Trihydrochloride	BIX01294 is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.
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 methyltransferas...
T2079	GSK126	GSK126 is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).
T2097	C7280948	C-7280948 is a PRMT1 inhibitor.
T2352	AMI-1	AMI-1 is an effective and selective Histone Methyltransferase (HMT) inhibitor (IC50: 3.0/8.8 μM, for yeast Hmt1p, and human PRMT1).
T2354	UNC0631	UNC0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).
T2435	EPZ011989	EPZ011989 is a effective, specific orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 Y646 and EZH2 wt; 15-fold selectivity over EZH1 and >3000-fold sel...
T2649	MI-2	MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
T3057	UNC1999	UNC1999 is a orally bioavailable, effective and specific inhibitor of EZH2 (IC50=2 nM) and EZH1 (IC50=45).
T3081	EPZ004777	EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
T3082	SGC0946	SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.
T3084	SGC707	SGC707 is a potent, selective, and cell-active allosteric inhibitor of PRMT3.
T3099	Pinometostat	EPZ5676 has been used in trials studying the treatment of Leukemia, Acute Leukemias, Acute Myeloid Leukemia, Myelodysplastic Syndrome, and Acute Lymphocytic Leu...
T3257	UNC0638	UNC0638 is an inhibitor of β-protein lysine methyltransferases G9a(IC50<15 nM) and GLP(IC50=19 nM) with excellent potency and selectivity over a wide range of ...
T3458	EED226	EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.
T3624	A-366	Potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50 = 3.3 nM). Exhibits >1000-fold selectivity for G9a/GLP over 21 other methyltransf...
T3896	Shanzhiside methyl ester	Shanzhiside methylester reduces neuropathic pain by activating spinal GLP-1 receptors and subsequently stimulating microglial β-endorphin expression via the p3...
T3984	GLP-1(7-36)	GLP-1 (7-36) amide is a peptide hormone released from intestinal L-cells upon nutrient consumption. It binds the GLP-1 receptor in the pancreas and displays var...
T4013	SGC2085 HCl	SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectiv...
T4021	UNC3866	UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen.
T4166	UNC-0642	UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).
T6059	GSK343	GSK343，a specific and effective EZH2 inhibitor (IC50=4 nM), exhibits 60 fold specificity activity against EZH1, and >1000 fold specificity activity against ot...
T6076	EPZ015666	EPZ015666 is an orally available inhibitor of PRMT5 enzymatic activity.
T6333	MM102	MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.
T6484	EI1	EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
T6790	BMS-911543	BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.
T6809	CPI-169	CPI-169 is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.
T6853	GSK591	GSK591，Alternative Names are EPZ015866, GSK3203591， is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).
T6857	HLCL-61 hydrochloride	HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
T6876	Liraglutide	Liraglutide is a long-acting GLP-1 receptor agonist.
T6879	LLY-507	LLY-507 is an effective, cell-active, and specific inhibitor of protein-lysine Methyltransferase SMYD2.
T6900	MS023	MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, ...
T4314	EPZ020411	EPZ020411 is a specific and effective inhibitor of PRMT6 (IC50=10 nM).
T4334	EPZ020411 2HCl (1700663-41-7(free base))	EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).
T4378	MS049	MS 049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC 50 of 34 nM and 43 nM, respectively.
T4393	MS049 2HCl (1502816-23-0(free base))	MS049 is a potent and selective inhibitor of PRMT4 (IC50 = 34 nM) and PRMT6 (IC50 = 43 nM). It is less active against additional type I PRMTs (IC50s = >130, >22...
T4343	A-196	A-196 is a potent and selective inhibitor of SUV420 h1 and SUV420 h2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over ot...
T4583	(R)-PFI-2 hydrochloride	PFI-2 hydrochloride is a potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 (IC50: 2 nM), 500 fold active than (S)-P...
T7089	SGC2085	SGC2085 is an effective and selective coactivator-associated arginine methyltransferase 1 (CARM1) inhibitor (IC50: 50 nM).
T5322	BCI-121	BCI-121 is a substrate-competitive SMYD3 inhibitor that inhibits the proliferation of the cancer cell.
T5605	EZM 2302	EZM2302 is a selective, and orally available arginine methyltransferase CARM1 inhibitor (IC50: 6 nM).
T5745	GSK3326595	GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).
T7157	XY1	XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), It is intended to be used as a negative...
T7305	JQEZ5	JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM).
T7378	BRD9539	BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2), also known as G9a, with an IC50 value of 6.3 μM
T7403	BAY-598	BAY-598 is a selective inhibitor of SMYD2 with IC50 values of 27 nM.
T7697	BIX-01294	BIX-01294 is an G9a Histone Methyltransferase inhibitor(IC50 : 1.9 μM).
TQ0058	MI-463	MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM).
TQ0069	MI-503	MI-503 is a highly effective and orally bioavailable inhibitor of the menin-mLL interaction.
TQ0100	AZ505	AZ505 is an effective and specific SMYD2 inhibitor (IC50: 0.12 μM).
TQ0232	UNC 0646	UNC0646 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...
TQ0263	EPZ031686	EPZ031686 is a selective and orally available SMYD3 inhibitor (IC50: 3 nM).
T8201	Gambogenic acid	Gambogenic acid is a natural product,is an effective inhibitor of EZH2,with anticancer activity.
T13780	MS1943	MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).
T12428	PF-06726304 acetate	PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity.
T12541	PRMT5-IN-1	PRMT5-IN-1 is a covalent inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50 of 11 nM for PRMT5/MEP50).
T11081	Dot1L-IN-1	The Ki value of DOT1L-in-1 is 2pm.It is a highly effective, selective and novel Dot1L inhibitor.
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...
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.
T11084	Dot1L-IN-5	Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.17 nM.
T10427	AZ505 ditrifluoroacetate	AZ505 ditrifluoroacetate is an effective and selective SMYD2 inhibitor (IC50: 0.12 μM).
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.
T8510	CPI-1205	CPI-1205 is a highly potent and selective inhibitor of EZH2(IC50 : 0.002 μM, EC50 : 0.032 μM) .
T15080	DC-05	DC-05 is an inhibitor of DNA methyltransferase 1 (DNMT1) (IC50: 10.3 μM; Kd: 1.09 μM).
T15194	EBI-2511	EBI-2511 is a highly potent and orally active inhibitor of EZH2 (IC50: 6 nM in Pfeffiera cell lines).
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...
T12939	SMYD2-IN-1	SMYD2-IN-1 is an inhibitor of SMYD2 (IC50 of 4.45 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).
T12943	SNDX-5613	SNDX-5613 is a potent and specific inhibitor of Menin-MLL(Ki of 0.149 nM and a cell based IC50 of 10-20 nM). SNDX-5613 can be used for the research of MLL-rearr...
T11131	DW14800	DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity.DW14800 is a protein arginin...
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 ...
T11436	GNA002	GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting prote...
T11486	GSK2807 Trifluoroacetate	GSK2807 Trifluoroacetate is a selective, potent and SAM-competitive inhibitor of SMYD3, with a Ki of 14 nM and an IC50 of 130 nM.
T11500L	GSK3368715 dihydrochloride	GSK3368715 dihydrochloride produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.GSK3368715 dihydrochloride ...
T11500	GSK3368715	GSK3368715 produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity. GSK3368715 is an orally active, reversible...
T13279	Valemetostat tosylate	Valemetostat tosylate is a dual inhibitor of EZH1/2, and used in the research of relapsed/refractory peripheral T-cell lymphoma.
T15624	JNJ-64619178	JNJ-64619178 has effective activity In lung cancer. JNJ-64619178 is a selective, orally active, and pseudo-irreversible inhibitor of protein arginine methyltran...
T16072	MI-538	MI-538 is an interaction between menin and MLL fusion proteins inhibitor(IC50 of 21 nM).
T10882	CPUY074020	CPUY074020 is a potent and orally bioavailable inhibitor of histone methyltransferase G9a (IC50: 2.18 μM) with anti-proliferative activity.
T15775	Lotilaner	Lotilaner is a parasiticide. It is used as a potent non-competitive antagonist of insects GABACl receptors (IC50 of 23.84 nM for Drosophila melanogaster GABA re...
T16435	PBIT	PBIT inhibits JARID1B histone demethylase (IC50 of about 3 μM). PBIT also inhibits JARID1A and JARID1C (IC50s of 6 μM and 4.9 μM, respectively). PBIT is a sp...
T12428L	PF-06726304	PF-06726304 shows robust antitumor growth activity. PF-06726304 is an effective and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZ...
T16577	PRMT5-IN-2	PRMT5-IN-2 is an inhibitor of protein arginine methyltransferase 5.
T17002	Tazemetostat hydrobromide	Tazemetostat hydrobromide is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2...
T17203	UNC0224	UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3, and JMJD2E. UNC0224 is a potent and selective histone methyltransferase G9a inhibitor (Ki: 2.6 nM, an I...
T17204	UNC0321	UNC0321 is inactive against SET7/9, SET8/PreSET7, PRMT3, and JMJD2E. UNC0321 is an effective and selective histone methyltransferase G9a inhibitor (Ki: 63 pM) a...
T22325	EPZ020411 2HCl	EPZ020411 is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 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...
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...
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 thera...