Histone Methyltransferase

Histone Methyltransferase
第页，共 4 页

货号	产品名	CAS号	信息
CSN26505	VTP50469	2169916-18-9	VTP-50469 is a novel, potent, selective, orally-available MeninMLL1 inhibitor, being effectively against MLL-rearranged and NPM1c+ leukemia, selectively killing cell lines with MLLrearrangements and NPM1c+ mutations.
CSN23177	UNC 0638 hydrate	1255517-77-1	UNC0638 is an inhibitor of protein lysine methyltransferases G9a and GLP with IC50 of < 15 nM, 19 nM, respectively.
CSN23170	TP-064	2080306-20-1	TP-064 is a potent and selective PRMT4 inhibitor. The in vitro activity of TP-064 includes inhibition of PRMT4 with IC50 < 10nM for methylation of H3 (1-25) and greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In cellular assays, TP-064 inhibits the methylation of MED12 with IC50 = 43 nM.
CSN23150	TC-E 5003	17328-16-4	TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor.
CSN23083	Ryuvidine	265312-55-8	Ryuvidine is an inhibitor of SETD8 with cellular activity. It also acts as a CDK4 inhibitor and inducer of the DNA damage response.
CSN20439	PRMT5 Inhibitor C17	330951-01-4	PRMT5 inhibitor C17 is a potent, selective, and cell active protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50 = 0.33 μM) exhibited a broad selectivity against a panel of other methyltransferases.
CSN26408	PF-06726304	1616287-82-1	PF-06726304 is a potent and selective EZH2 inhibitor with Ki value of 0.7 nM.
CSN27839	MR837	1210906-48-1	NSD2-PWWP1 antagonist 3f can bind to the NSD2-PWWP1 domain with Kd value of 3.4μM and abrogates histone H3K36me2 binding to the PWWP1 domain in cells.
CSN51119	MS37452	423748-02-1	MS37452 compete against H3K27me3 binding through interactions with key residues in the methyl-lysine binding pocket of CBX7ChD. It derepresses transcription of Polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells.
CSN27203	MS1943	2225938-17-8	MS1943 is a first-in-class EZH2 selective degrader that effectively reduces EZH2 levels in cells.
CSN19233	MS049 dihydrochloride	2095432-59-8	MS049 2HCl is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.
CSN20284	MM-589 TFA	2253167-09-6	MM-589 trifluoroacetate is a potent inhibitor of the WD repeat domain 5 protein (WDR5)–mixed lineage leukemia (MLL) interaction, and may yield a therapy for acute leukemia.
CSN20283	MM-589	2097887-20-0	MM-589 is a potent inhibitor of the WD repeat domain 5 protein (WDR5)–mixed lineage leukemia (MLL) interaction, and may yield a therapy for acute leukemia.
CSN26672	M-808	2377335-74-3	M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor, with IC50 values of 1 nM and 4 nM in MV4;11 cells and MOLM-13 cells, respectively[1].
CSN22449	LLY-283	2040291-27-6	LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity.
CSN22869	JQEZ5	1913252-04-6	JQEZ5 is a potent and selective SAM-competitive EZH2 lysine methyltransferase inhibitor with IC50 of 11 nM.
CSN29543	Onametostat	2086772-26-9	JNJ-64619178 is a selective, orally active, and pseudo-irreversible inhibitor of protein arginine methyltransferase 5 (IC50: 0.14 nM). It has effective activity In lung cancer.
CSN26479	GSK3368715	1629013-22-4	GSK3368715, aslo known as EPZ019997, is a potent, reversible type I PRMT inhibitor with anti-tumor effects in human cancer models. Inhibition of PRMT5, the predominant type II PRMT, produces synergistic cancer cell growth inhibition when combined with GSK3368715. Interestingly, deletion of the methylthioadenosine phosphorylase gene (MTAP) results in accumulation of the metabolite 2-methylthioadenosine, an endogenous inhibitor of PRMT5, and correlates with sensitivity to GSK3368715 in cell lines.
CSN26480	GSK3368715 HCl	2227587-25-7	GSK3368715 dihydrochloride is a novel potent type-I protein arginine methyltransferases (PRMTs) inhibitor.
CSN51125	GSK3368715 dihydrochloride	1628925-77-8	GSK3368715 2HCl is a novel potent type-I protein arginine methyltransferases (PRMTs) inhibitor.
CSN23320	GSK3326595	1616392-22-3	GSK3326595 is a potent, specific and reversible PRMT5 inhibitor which can decrease the levels of both monomethylated and dimethylated arginine residues in histones H2A, H3 and H4.
CSN22899	GSK2807 Trifluoroacetate	2245255-66-5	GSK2807 Trifluoroacetate is a SMYD3 SAM-competitive inhibitor with Ki of 14 nM.
CSN26668	Furamidine	73819-26-8	Furamidine, also known as DB75, is a cell-permeable inhibitor of protein arginine methyltransferase 1 (PRMT1) that is selective for PRMT1. Furamidine (DB75) binds to strings of AT base pair sequences in DNA′s minor groove. Furamidine was originally developed as an anti-parasitic compound for a variety of diseases including Chagas′ disease. Furamidine targets the enzyme active site and is primarily competitive with the substrate and noncompetitive toward the cofactor. Furthermore, cellular studies revealed that 1 is cell membrane permeable and effectively inhibits intracellular PRMT1 activity and blocks cell proliferation in leukemia cell lines with different genetic lesions.
CSN22826	Furamidine dihydrochloride	55368-40-6	Furamidine 2HCl is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with IC50 of 9.4 μM.
CSN26548	EML741	2328074-38-8	for G9a. 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 barrier penetrated[1].
CSN22212	EZM 2302	1628830-21-6	EZM 2302 is the first potent and selective inhibitor of CARM1 enzymatic activity with IC50 value of 6 nM.
CSN26674	EZH2-IN-2	2238821-31-1	EZH2-IN-2 is a EZH2 inhibitor extracted from patent WO2018133795A1, Compound Example 69, with an IC50 of 64 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity[1].
CSN18964	EPZ031686	2095161-11-6	EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a K_i=1.2 nM and 1.1 nM respectively.
CSN19213	EPZ020411 2HCl	2095432-47-4	EPZ020411 2HCl is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.
CSN19263	EPZ011989 Hydrochloride	2095432-26-9	EPZ011989 HCl is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of < 3 nM.
CSN21098	EBI-2511	2098546-05-3	EBI-2511 is a Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin’s Lymphoma. EBI-2511 showed enzymatic activity and cellular activity of 4.0 and 6.0nM, respectively. EBI-2511 demonstrated excellent in vivo efficacy in Pfeiffer tumor Xenograft models in mouse and is under preclinical development for the treatment of cancers associated with EZH2 mutations.
CSN26671	CMP-5 hydrochloride	1030021-40-9	CMP5 is a potent and selective PRMT5 Inhibitor. CMP5 showed to occupy hPRMT5 catalytic site and block symmetrically dimethylated S2Me-H4R3 & S2Me-H3R8 with no effect on the asymmetric methylation of H4R3 in lymphoblastoid cell lines at 40 µM. CMP-5 shows promise as a novel therapeutic approach for B-cell lymphomas.
CSN26670	CMP-5	880813-42-3	CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected[1][2].
CSN19229	Chaetocin	28097-03-2	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 and Neurospora crassa DIM5, respectively. It also inhibits thioredoxin reductase (TrxR) with an IC50 of 4 μM.
CSN18958	CARM1-IN-1 hydrochloride	2070018-31-2	CARM1-IN-1 HCl is a potent and specific CARM1 (Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 μM and shows very low activity against PRMT1 and SET7 (IC50 > 600 μM).
CSN23850	BCI-121	432529-82-3	BCI-121 (BCI121) is a substrate-competitive inhibitor of SMYD3 that inhibits SMYD3-substrate interaction and chromatin recruitment It can significantly reduce the proliferation of various cancer cells.
CSN22321	BAY-598	1906919-67-2	BAY-598 is an inhibitor of SMYD2. It can inhibit in vitro methylation of p53 at lysine 370 with IC50 value of 27 nM.
CSN27520	AMI-1 free acid	134-47-4	AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
CSN20242	A-893	1868232-32-9	A-893 is a potent and selective SMYD2 inhibitor (IC50: 2.8 nM).
CSN21388	A-395	2089148-72-9	A-395 is a antagonist of Polycomb repressive complex 2 (PRC2) protein–protein interactions that potently inhibits the trimeric PRC2 complex (EZH2–EED–SUZ12) with an IC50 of 18 nM.
CSN19081	A-196	1982372-88-2	A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50s of 25 and 144 nM respectively.
CSN28554	UNC6852	2688842-08-0
CSN28554	UNC6852	2688842-08-0
CSN42715	OTS186935	2093400-18-9
CSN51379	EZH2-IN-6	2702269-27-8
CSN51380	PRMT5-IN-15	2410637-87-3
CSN51430	SGC3027	2624313-13-7
CSN67084	TM2-115	1197196-47-6

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Histone Methyltransferase
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