Histone Methyltransferase

信号通路图

研究领域

抑制剂选择性比较
溶解性比较

目录号	产品目录	溶解度(25°C)
目录号	产品目录	水	DMSO	酒精
S7062	Pinometostat (EPZ5676)	<1 mg/mL	100 mg/mL	92 mg/mL
S7004	EPZ005687	<1 mg/mL	2 mg/mL	<1 mg/mL
S7164	GSK343	<1 mg/mL	1 mg/mL	4 mg/mL
S8006	BIX 01294	98 mg/mL	98 mg/mL	8 mg/mL
S7128	Tazemetostat (EPZ-6438)	<1 mg/mL	5 mg/mL	<1 mg/mL
S8702	EBI-2511	<1 mg/mL	30 mg/mL	13 mg/mL
S5445	AMI-1, free acid	-1 mg/mL	20 mg/mL	-1 mg/mL
S7120	3-deazaneplanocin A (DZNeP) HCl	52 mg/mL	52 mg/mL	<1 mg/mL
S7165	UNC1999	<1 mg/mL	20 mg/mL	50 mg/mL
S7265	MM-102	100 mg/mL	100 mg/mL	100 mg/mL
S7079	SGC 0946	<1 mg/mL	100 mg/mL	100 mg/mL
S3147	Entacapone	<1 mg/mL	61 mg/mL	2 mg/mL
S8071	UNC0638	6 mg/mL	100 mg/mL	100 mg/mL
S8353	CPI-1205	<1 mg/mL	100 mg/mL	100 mg/mL
S7570	UNC0379	<1 mg/mL	82 mg/mL	<1 mg/mL
S7748	EPZ015666(GSK3235025)	<1 mg/mL	60 mg/mL	48 mg/mL
S8147	MS049	56 mg/mL	56 mg/mL	50 mg/mL
S7230	UNC0642	<1 mg/mL	100 mg/mL	100 mg/mL
S8340	SGC2085	<1 mg/mL	62 mg/mL	62 mg/mL
S7294	PFI-2 HCl	4 mg/mL	99 mg/mL	25 mg/mL
S7983	A-196	<1 mg/mL	15 mg/mL	12 mg/mL
S4589	Amodiaquine dihydrochloride dihydrate	29 mg/mL	92 mg/mL	<1 mg/mL
S8479	LLY-283	<1 mg/mL	68 mg/mL	68 mg/mL
S7820	EPZ020411 2HCl	81 mg/mL	100 mg/mL	100 mg/mL
S7816	MI-463	<1 mg/mL	96 mg/mL	22 mg/mL
S7832	SGC707	<1 mg/mL	59 mg/mL	59 mg/mL
S7817	MI-503	<1 mg/mL	100 mg/mL	15 mg/mL
S8112	MS023	<1 mg/mL	57 mg/mL	57 mg/mL
S8068	Chaetocin	<1 mg/mL	100 mg/mL	<1 mg/mL
S7619	MI-3 (Menin-MLL Inhibitor)	<1 mg/mL	19 mg/mL	19 mg/mL
S7572	A-366	<1 mg/mL	65 mg/mL	65 mg/mL
S8664	GSK3326595 (EPZ015938)	<1 mg/mL	90 mg/mL	90 mg/mL
S7591	BRD4770	<1 mg/mL	27 mg/mL	<1 mg/mL
S7805	EPZ011989	<1 mg/mL	<1 mg/mL	100 mg/mL
S7618	MI-2 (Menin-MLL Inhibitor)	<1 mg/mL	75 mg/mL	75 mg/mL
S7575	LLY-507	<1 mg/mL	100 mg/mL	22 mg/mL
S8111	GSK591	<1 mg/mL	76 mg/mL	76 mg/mL
S8209	HLCL-61 HCL	<1 mg/mL	76 mg/mL	76 mg/mL
S8494	PF-06726304	<1 mg/mL	10 mg/mL	22 mg/mL
S7611	EI1	<1 mg/mL	42 mg/mL	<1 mg/mL
S8624	JNJ-64619178	-1 mg/mL	100 mg/mL	-1 mg/mL
S7804	GSK503	<1 mg/mL	100 mg/mL	26 mg/mL
S7353	EPZ004777	<1 mg/mL	100 mg/mL	100 mg/mL
S7061	GSK126	<1 mg/mL	3 mg/mL	<1 mg/mL
S7656	CPI-360	<1 mg/mL	20 mg/mL	18 mg/mL
S7616	CPI-169	<1 mg/mL	100 mg/mL	100 mg/mL
S7884	AMI-1	10 mg/mL	100 mg/mL	<1 mg/mL
S7815	MI-136	<1 mg/mL	94 mg/mL	94 mg/mL
S7833	OICR-9429	<1 mg/mL	38 mg/mL	14 mg/mL
S8359	UNC3866	<1 mg/mL	100 mg/mL	46 mg/mL

Histone Methyltransferase产品

所有产品 Histone Methyltransferase抑制剂(49) Histone Methyltransferase拮抗剂(2) 新Histone Methyltransferase产品

产品目录	产品描述	文献引用	实验数据
S7062	Pinometostat (EPZ5676) Pinometostat (EPZ5676)是一种蛋白甲基转移酶DOT1L的S-腺苷甲硫氨酸(SAM)竞争性抑制剂，无细胞试验中K_i为80 pM，比作用于所有其他测试的PMTs选择性高37000倍以上，抑制肿瘤中H3K79甲基化。Phase 1。	Haematologica, 2018, 103(7):1110-1123 Theranostics, 2018, 8(16):4359-4371 Cell Rep, 2014, 9(3):1163-70	Treatment of c-Kit+ bone marrow (BM) cells from Setd2^f/f/Vav1-Cre mice with JQ1 500nM, EPZ-5676 1uM, BAY 1143572 400 nM for 24 h. Then cells were collected to determine the proteins levels of RNA pol II (Ser2P), pol II (Ser5P), Gata1, Gata3, Myc, and β-actin by immunoblotting.
S7004	EPZ005687 EPZ005687是一种有效的，选择性EZH2抑制剂，无细胞试验中K_i为24 nM，比作用于EZH1选择性高50倍，比作用于15种其他蛋白甲基转移酶选择性高500倍。	Nature, 2018, 560(7718):372-376 Oncogene, 2015, 10.1038/onc.2015.38 J Biol Chem, 2017, pii: jbc.M116.765800	Representative images of OPCs treated for 72 h with the indicated EZH2 inhibitors. All treatments are at 2 μM. Scale bar, 100 μm.
S7164	GSK343 GSK343是一种有效的，选择性EZH2抑制剂，无细胞试验中IC50为4 nM，比作用于EZH1选择性高60倍，比作用于其他组蛋白甲基转移酶选择性高1000倍以上。	Nucleic Acids Res, 2016, 44(16):7659-72 Mol Cancer, 2017, 16(1):5 Oncogene, 2015, 10.1038/onc.2015.38	Representative confocal microscopy images of oocytes with DZNep or GSK343 treatment. The oocytes presented with a typical barrel-shaped spindle and well-aligned chromosomes on the metaphase plate not only in DZNep or GSK343 treated group but also in the control group. Spindle was recognized by α-tubulin (green) and DNA was recognized by PI (Propidium iodide, red). Scale bar = 4 μm.
S8006	BIX 01294 BIX01294是一种G9a histone methyltransferase抑制剂，无细胞试验中IC50为2.7 μM，降低大部分组蛋白H3K9me2，也微弱抑制GLP（主要是H3K9me3），对其他组蛋白甲基转移酶没有显著的抑制活性。	Cancer Res, 2015, 75(11):2375-86 J Pineal Res, 2018, 65(2):e12497 Hum Pathol, 2018, 72:117-126	(H) Fold change of miR-200c expression in MCF7 cells under leptin and S3I-201/BIX01294 treatment (n=3, asterisk indicates P<0.05). Error bars denote ±SD.
S7128	Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438)是一种有效的，选择性EZH2抑制剂，无细胞试验中K_i 和 IC50分别为2.5 nM 和 11 nM，比作用于EZH1选择性高35倍，比作用于14种其他HMT选择性高4500多倍。	Nature, 2018, 560(7718):372-376 Cell, 2018, 175(1):186-199 J Pathol, 2017, 242(3):371-383	EZH2i-induced H3K27ac level change in cancer cells. Cells were treated with 1 mM EPZ-6438 and 1 mM GSK126 for 6 days, respectively. H3K27ac was detected by immunoblotting. Lysates from each cell line were blotted individually. EPZ: EPZ-6438.
S8702^New	EBI-2511 EBI-2511是一种有效的、具有口服活性的EZH2抑制剂，对EZH2(A667G)的IC50值为4 nM。
S5445^New	AMI-1, free acid AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.
S7120	3-deazaneplanocin A (DZNeP) HCl 3-deazaneplanocin A (DZNeP)HCl，一种腺苷类似物，是竞争性S-adenosylhomocysteine hydrolase抑制剂，无细胞试验中K_i为50 pM。	J Infect Dis, 2016, 10.1093/infdis/jiw226 J Virol, 2018, 10.1128/JVI.00909-18 Antiviral Res, 2016, 133:119-29	H3K27me3 inhibitors inducing cell differentiation in the MDS-derived erythroid/myeloid cell line and primary MDS bone marrow cells via reducing H3K27me3 and increasing the expressions of PU.1 and its downstream genes. (a) ChIP experiments show a marked decrease in H3K27me3 at the PU.1 enhancer in the OCI-M2 cells treated with DZNep, compared with that in the cells treated with dimethyl sulfoxide (DMSO). (b) RT-PCRs show a significant increase in the expression of PU.1 mRNA in the OCI-M2 cells treated with DZNep in a dose-dependent manner. (c) Flow cytometric studies show that an increase in the expression of glycophorin A/B, a marker associated with erythroid differentiation, in the OCI-M2 cells treated with 0.25 μM of DZNep for 6 days. Red, isotype control; blue, no drug treatment (DMSO only); green, plus drug. (d) Increased PU.1 mRNA expression in primary MDS bone marrow cells treated with DZNep, compared with that in DMSO control. (e) Increased CD18 mRNA expression in primary MDS bone marrow cells treated with DZNep, compared with that in DMSO control. The primary bone marrow cells were from three cytogenetically normal MDS patients, which had marked trilineage dysplasia with varying numbers of blasts (case-1 with 10% blasts, case-2 with 4.6% blasts and case-3 with 11% blasts). The MDS bone marrow cells were treated with 1 μM DZNep or DMSO (control) for 24 h. The levels of PU.1 and CD18 mRNAs were measured by Q-RT-PCRs, while TBP mRNA was used for the internal normalization
S7165	UNC1999 UNC1999一种有效的具有口服活性的EZH2和EZH1选择性抑制剂，无细胞试验中IC50分别为2 nM和45 nM，对广泛表观遗传学相关或不相关的靶点选择性大于1000倍。	Nature, 2018, 560(7718):372-376 Oncogene, 2015, 10.1038/onc.2015.38 J Pathol, 2018, 245(4):433-444	Ex vivo growth of the SCLC PDX LX92 is significantly inhibited by the EZH2 inhibitors EPZ-5687, GSK343 and UNC1999 as measured by resazurin conversion (two-way analysis of variance, adjusted for multiple comparisons by the method of Dunnet).
S7265	MM-102 MM-102是一个高亲和力的多肽模拟的MLL1抑制剂，无细胞试验中IC50为0.4 μM。	Mol Cell Biol, 2015, 36(4):615-27 Biochem Biophys Res Commun, 2016, 469(1):108-13 Cell Physiol Biochem, 2018, 45(4):1529-1540	(D) ChIP-qPCR analysis of the H3K4me3 levels in hESCs synchronized in mitosis with or without MLL1/2 inhibitors. DMSO, cells treated with DMSO only; Noc, cells blocked in mitosis with nocodazole; Noc + MLL Inh, cells blocked in mitosis with nocodazole in the presence of Mi-2 and MM-102 (20 μM each). Values for percent input are normalized to the IgG control (n = 2). One-way analysis of variance followed by Tukey's test for multiple comparisons was performed. , P < 10⁻²; **, P < 10⁻⁵; ns, not significant. (E) Reverse transcription-qPCR analysis of RNA expression levels for bivalent genes after induction of differentiation in unsynchronized H9 ES cells pretreated with MLL inhibitors. Differentiation was induced using E6 medium containing 1 μM RA per 24 h. DMSO, cells pretreated with DMSO only; MLL Inh, cells pretreated with Mi-2 and MM-102 (20 μM each) for 24 h. Unpaired parametric t test with Welch's corrections was performed. Two-tailed P values were calculated. , P < 10⁻²; , P < 10⁻³; *, P < 10⁻⁴; ns, not significant. Log2 RNA levels were normalized against HPRT1 RNA levels and expressed as fold change between undifferentiated and differentiated cells.
S7079	SGC 0946 SGC 0946是一种高效的，选择性的DOT1L甲基转移酶抑制剂，无细胞试验中IC50为0.3 nM，对一系列12 PMTs和DNMT1没有活性。
S3147	Entacapone Entacapone抑制儿茶酚-O-甲基转移酶(COMT)活性，IC50为151 nM。
S8071	UNC0638 UNC0638是一种有效的选择性的组蛋白赖氨酸甲基转移酶（HMTase）抑制剂，作用于G9a和GLP，IC50分别为< 15 nM和19 nM，有效且选择性地作用于多种表观遗传和非表观遗传靶点。
S8607	JQ-EZ-05 (JQEZ5) JQ-EZ-05是可逆的、特异的EZH1/2抑制剂。
S8353	CPI-1205 CPI-1205是具有口服生物活性的选择性组蛋白赖氨酸甲基转移酶EZH2的抑制剂，对EZH2和EZH1的IC50分别为2 nM和52 nM。它具有潜在的抗肿瘤活性。
S7570	UNC0379 UNC0379 是一种选择性，底物竞争性N-lysine methyltransferase SETD8抑制剂，IC50为7.9 μM，选择性比其他15种甲基转移酶高。	Mol Cancer Ther, 2018, 17(7):1585-1594
S7748	EPZ015666(GSK3235025) EPZ015666(GSK3235025) 是一种有效的，选择性且口服生物有效的 PRMT5 抑制剂，K_i 为 5 nM，选择性比其它 PMTs 高 20,000多倍。	J Cell Mol Med, 2017, 21(4):781-790 Cell Signal, 2017, 34:55-65	(B) Effect of EPZ015666 on nuclear translocation of p65. Middle panel showed a representative photo of IF staining of p65 localization (green). Nuclei were stained with DAPI.
S8147	MS049 MS049是有效的、选择性的PRMT4和PRMT6抑制剂，IC50分别为34 nM和43 nM。
S7230	UNC0642 UNC0642是一种有效的、选择性的histone methyltransferases G9a/GLP抑制剂，对G9a和GLP的IC50均小于2.5 nM。对G9a和GLP的选择性比其他激酶、GPCRs、转运体和离子通道高300倍以上。
S8340	SGC2085 SGC2085是一种有效的、选择性的Coactivator Associated Arginine Methyltransferase 1 (CARM1)抑制剂，IC50为50 nM，比对其他PRMTs的选择性高100倍以上。
S7294	PFI-2 HCl PFI-2是一种强效的，有选择性和细胞活性的lysine methyltransferase SETD7抑制剂，K_{i (app)}和IC50分别为0.33 nM 和2 nM，比其他甲基转移酶和非后生的靶点高出1000倍的选择性。
S7983	A-196 A-196是一种有效的、选择性的SUV420H1和SUV420H2抑制剂，IC50s分别为0.025 μM和0.144 μM。选择性比对其他组蛋白转移酶以及非表观遗传靶标高100倍以上。
S4589	Amodiaquine dihydrochloride dihydrate Amodiaquine在人红细胞中是一种有效的、非竞争性的组胺N-甲基转移酶抑制剂，其Ki值为18.6 nM。它也被用作抗疟疾药和消炎药。
S8479	LLY-283 LLY-283是有效的、选择性的SAM竞争性的化学探针，靶向PRMT5。它抑制PRMT5活性，抑制其对H4R3衍生的肽段底物的甲基化，IC50为20 nM。其对PRMT5的选择性比对其他组蛋白甲基转移酶和非表观遗传靶点的选择性高100倍以上。
S7820	EPZ020411 2HCl EPZ020411是有效的、选择性的PRMT6小分子抑制剂，IC50为10 nM。
S7816	MI-463 MI-463是Menin-MLL interaction的有效抑制剂，IC50为15.3 nM。
S7832	SGC707 SGC707是一种有效的，选择性的，且具有细胞活性的蛋白精氨酸甲基转移酶 3 (PRMT3)变构抑制剂，IC50 和 K_d分别为31 nM 和 53 nM。
S7817	MI-503 MI-503是一种有效的、选择性的Menin-MLL抑制剂，IC50为14.7 nM。在人类MLL白血病细胞系中，具有显著的生长抑制效果（GI=250 nM-570 nM），但是在不具有MLL易位的人类白血病细胞中，效果甚微。
S8112	MS023 MS023是一类高效选择性并且有细胞活性的I型PRMT抑制剂，其对PRMT1, PRMT3, PRMT4, PRMT6和PRMT8的IC50分别为30 nM, 119 nM, 83 nM, 4 nM, 和5 nM。
S8068	Chaetocin Chaetocin，一类来自毛壳菌属的天然产物，是一类 histone methyltransferase抑制剂，其对dSU(VAR)3-9，小鼠G9a和粗糙链孢霉 DIM5的IC50分别为0.8 μM, 2.5 μM和3 μM。
S7619	MI-3 (Menin-MLL Inhibitor) MI-3 (Menin-MLL Inhibitor)是一种强效的menin-MLL相互作用抑制剂，IC50为 648 nM。
S7572	A-366 A-366是一种有效的、选择性的G9a/GLP组蛋白甲基转移酶抑制剂，IC50为3.3 nM。对G9a/GLP的选择性比21个其他甲基转移酶高1000倍以上。
S8664	GSK3326595 (EPZ015938) GSK3326595 (EPZ015938)是一种具有口服活性的、有效的、选择性protein arginine methyltransferase 5 (PRMT5)抑制剂，在体内外有效地抑制肿瘤生长。
S7591	BRD4770 BRD4770是一种histone methyltransferase G9a抑制剂，其IC50为6.3 μM，并且会诱导细胞死亡。	Hum Pathol, 2018, 72:117-126
S7805	EPZ011989 EPZ011989是一种有效的、选择性的、具有口服活性的EZH2抑制剂，Ki值<3 nM。	J Cancer, 2018, 9(20):3787-3796
S7618	MI-2 (Menin-MLL Inhibitor) MI-2 (Menin-MLL Inhibitor)是一种有效的menin-MLL相互作用抑制剂，IC50为446 nM。	Mol Cell Biol, 2015, 36(4):615-27
S7575	LLY-507 LLY-507是一种具有细胞活性的和选择性的、有效的蛋白质赖氨酸甲基转移酶SMYD2的抑制剂。
S8111	GSK591 GSK591 (EPZ015866,GSK3203591)是一种有效的、选择性PRMT5抑制剂。	Cancer Med, 2018, 7(3):869-882	Treatment of HCC cells with 500 nmol/L GSK591 for 4 days led to significant loss of PRMT5-catalyzed methylarginine on H4 (H4R3me2s), the upregulation of BTG2, and the phosphorylation of ERK. Inhibition of ERK phosphorylation by PD184352 treatment reversed these effects. H4R3me2s was used to detect the PRMT5 activity. Histone 3 was used as nuclear loading control.
S8209	HLCL-61 HCL HLCL-61 hydrochloride是一种有效的、选择性PRMT5抑制剂，用作治疗急性髓性白血病。
S8494	PF-06726304 PF-06726304是选择性EZH2抑制剂，对WT EZH2和EZH2(Y641N)的Ki值分别为0.7 nM和3 nM。抑制H3K27me3的IC50为15 nM。
S7611	EI1 EI1是一种有效的选择性EZH2抑制剂，对EZH2 (WT)和EZH2 (Y641F)的IC50分别为15 nM和13 nM。	Mol Cancer, 2017, 10.1186/s12943-016-0575-6 Oncotarget, 2015, 6(32):32410-25	EZH2 inhibitors EI1 or GSK343 are applied in MDA-MB-231 breast cancer cells with NBAT1 over-expression. The invasion suppression effects of NBAT1 was reversed by concomitant EZH2 inhibitors.
S8624	JNJ-64619178 JNJ-64619178是PRMT5抑制剂，具有较高的选择性和效力（PRMT5-MEP-50, IC50=0.14 nM）、良好的药代动力学特性以及安全性。
S7804	GSK503 GSK503是一种有效的特异性EZH2甲基转移酶抑制剂。	J Pathol, 2018, 245(4):433-444 Front Immunol, 2016, 7:496	LC3B‐II levels are increased following 120 h treatment of GSK503 (G, CRMM1 and CRMM2 at 10 μm, and CM2005.1 at 15 μm) or UNC1999 (U, 6 μm).
S7353	EPZ004777 EPZ004777是一种有效的，选择性的DOT1L抑制剂，无细胞试验中IC50为0.4 nM。	Theranostics, 2018, 8(16):4359-4371 Int J Cancer, 2017, 141(2):324-335 FEBS J, 2017, 10.1111/febs.14060	THP-1 cells were treated with MI-3 (6.25 μM, 6 days), GSK126 (5 μM, 6 days), or EPZ004777 (5 μM, 6 days), with orwithout PMA (50 ng/mL, 12 h), and surface expression of CD11b was determined by ﬂow cytometric analysis. The data are representedas the mean ± SD, n = 3. THP-1 cells were collected for Wright-Giemsa staining.
S7061	GSK126 GSK126 是一种有效的，高选择性EZH2 methyltransferase抑制剂，IC50为9.9 nM，对 EZH2 的选择性比其他20种人甲基转移酶高1000多倍。	Nature, 2019, 566(7743):270-274 Nature, 2019, 566(7744):344-349 Mol Cancer, 2017, 16(1):22	HeLa cells were transfected with NS (nonspecific) or EZH2-specific siRNA for 48 h with protease inhibitors (10 μM E64 and 10 μM pepstatin-A). Cells were stained with LC3B antibody (green) and DAPI, and observed under confocal microscopy for LC3B puncta. Scale bars: 10 μm
S7656	CPI-360 CPI-360是一种有效的，选择性的，且SAM竞争性EZH1抑制剂，IC50为102.3 nM，选择性比作用于其它甲基转移酶高100多倍。
S7616	CPI-169 CPI-169是一种有效的选择性EZH2抑制剂，作用于EZH2 WT，EZH2 Y641N，和EZH1的IC50分别为0.24 nM，0.51 nM，和6.1 nM。
S7884	AMI-1 AMI-1是一种有效的特异性Histone Methyltransferase (HMT)抑制剂，对酵母 Hmt1p 和人 PRMT1 的IC50分别为 3.0 μM 和 8.8 μM。	Nitric Oxide, 2017, 67:58-67	Effects of microinjection of AMI-1 into the RVLM on cardiovascular activity in the Ang II-induced hypertensive rats. The representative original tracings (A)
S7815	MI-136 MI-136抑制DHT所诱导的雄激素受体(AR)靶向基因的表达。
S7833	OICR-9429 OICR-9429是一种有效的WDR5-MLL、WDR5-Histone3相互作用的拮抗剂，能在体外实验中降低急性髓性白血病细胞的活性。它与WDR5高亲和结合，Kd值为93 ± 28 nM。	Theranostics, 2018, 8(18):5143-5158	(F) Real-time PCR analysis showed the VEGFA mRNA expression in the HOXC10-overexpressing glioma cells treated with vehicle or 1 μM OICR-9429 for 2 days. (G) ChIP-qPCR enrichments of H3K4me3, polymerase II or IgG on VEGFA promoter region 3 in the HOXC10-overexpressing glioma cells treated with vehicle or 1 μM OICR-9429 for 2 days. All the assays shown in the figure were independently replicated three times. Error bars, SD. * P < 0.05.
S8359	UNC3866 UNC3866是染色质域的多梳蛋白家族CBX和CDY的甲基赖氨酸阅读功能拮抗剂。它与CBX4和CBX7的染色质域有效结合，Kd值约为100 nM, 对CBX4和CBX7的选择性分别是对其他CBX和CDY染色质域的6倍和18倍。

产品目录	产品描述	文献引用	实验数据
S7062	Pinometostat (EPZ5676) Pinometostat (EPZ5676)是一种蛋白甲基转移酶DOT1L的S-腺苷甲硫氨酸(SAM)竞争性抑制剂，无细胞试验中K_i为80 pM，比作用于所有其他测试的PMTs选择性高37000倍以上，抑制肿瘤中H3K79甲基化。Phase 1。	Haematologica, 2018, 103(7):1110-1123 Theranostics, 2018, 8(16):4359-4371 Cell Rep, 2014, 9(3):1163-70	Treatment of c-Kit+ bone marrow (BM) cells from Setd2^f/f/Vav1-Cre mice with JQ1 500nM, EPZ-5676 1uM, BAY 1143572 400 nM for 24 h. Then cells were collected to determine the proteins levels of RNA pol II (Ser2P), pol II (Ser5P), Gata1, Gata3, Myc, and β-actin by immunoblotting.
S7004	EPZ005687 EPZ005687是一种有效的，选择性EZH2抑制剂，无细胞试验中K_i为24 nM，比作用于EZH1选择性高50倍，比作用于15种其他蛋白甲基转移酶选择性高500倍。	Nature, 2018, 560(7718):372-376 Oncogene, 2015, 10.1038/onc.2015.38 J Biol Chem, 2017, pii: jbc.M116.765800	Representative images of OPCs treated for 72 h with the indicated EZH2 inhibitors. All treatments are at 2 μM. Scale bar, 100 μm.
S7164	GSK343 GSK343是一种有效的，选择性EZH2抑制剂，无细胞试验中IC50为4 nM，比作用于EZH1选择性高60倍，比作用于其他组蛋白甲基转移酶选择性高1000倍以上。	Nucleic Acids Res, 2016, 44(16):7659-72 Mol Cancer, 2017, 16(1):5 Oncogene, 2015, 10.1038/onc.2015.38	Representative confocal microscopy images of oocytes with DZNep or GSK343 treatment. The oocytes presented with a typical barrel-shaped spindle and well-aligned chromosomes on the metaphase plate not only in DZNep or GSK343 treated group but also in the control group. Spindle was recognized by α-tubulin (green) and DNA was recognized by PI (Propidium iodide, red). Scale bar = 4 μm.
S8006	BIX 01294 BIX01294是一种G9a histone methyltransferase抑制剂，无细胞试验中IC50为2.7 μM，降低大部分组蛋白H3K9me2，也微弱抑制GLP（主要是H3K9me3），对其他组蛋白甲基转移酶没有显著的抑制活性。	Cancer Res, 2015, 75(11):2375-86 J Pineal Res, 2018, 65(2):e12497 Hum Pathol, 2018, 72:117-126	(H) Fold change of miR-200c expression in MCF7 cells under leptin and S3I-201/BIX01294 treatment (n=3, asterisk indicates P<0.05). Error bars denote ±SD.
S7128	Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438)是一种有效的，选择性EZH2抑制剂，无细胞试验中K_i 和 IC50分别为2.5 nM 和 11 nM，比作用于EZH1选择性高35倍，比作用于14种其他HMT选择性高4500多倍。	Nature, 2018, 560(7718):372-376 Cell, 2018, 175(1):186-199 J Pathol, 2017, 242(3):371-383	EZH2i-induced H3K27ac level change in cancer cells. Cells were treated with 1 mM EPZ-6438 and 1 mM GSK126 for 6 days, respectively. H3K27ac was detected by immunoblotting. Lysates from each cell line were blotted individually. EPZ: EPZ-6438.
S8702^New	EBI-2511 EBI-2511是一种有效的、具有口服活性的EZH2抑制剂，对EZH2(A667G)的IC50值为4 nM。
S5445^New	AMI-1, free acid AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.
S7120	3-deazaneplanocin A (DZNeP) HCl 3-deazaneplanocin A (DZNeP)HCl，一种腺苷类似物，是竞争性S-adenosylhomocysteine hydrolase抑制剂，无细胞试验中K_i为50 pM。	J Infect Dis, 2016, 10.1093/infdis/jiw226 J Virol, 2018, 10.1128/JVI.00909-18 Antiviral Res, 2016, 133:119-29	H3K27me3 inhibitors inducing cell differentiation in the MDS-derived erythroid/myeloid cell line and primary MDS bone marrow cells via reducing H3K27me3 and increasing the expressions of PU.1 and its downstream genes. (a) ChIP experiments show a marked decrease in H3K27me3 at the PU.1 enhancer in the OCI-M2 cells treated with DZNep, compared with that in the cells treated with dimethyl sulfoxide (DMSO). (b) RT-PCRs show a significant increase in the expression of PU.1 mRNA in the OCI-M2 cells treated with DZNep in a dose-dependent manner. (c) Flow cytometric studies show that an increase in the expression of glycophorin A/B, a marker associated with erythroid differentiation, in the OCI-M2 cells treated with 0.25 μM of DZNep for 6 days. Red, isotype control; blue, no drug treatment (DMSO only); green, plus drug. (d) Increased PU.1 mRNA expression in primary MDS bone marrow cells treated with DZNep, compared with that in DMSO control. (e) Increased CD18 mRNA expression in primary MDS bone marrow cells treated with DZNep, compared with that in DMSO control. The primary bone marrow cells were from three cytogenetically normal MDS patients, which had marked trilineage dysplasia with varying numbers of blasts (case-1 with 10% blasts, case-2 with 4.6% blasts and case-3 with 11% blasts). The MDS bone marrow cells were treated with 1 μM DZNep or DMSO (control) for 24 h. The levels of PU.1 and CD18 mRNAs were measured by Q-RT-PCRs, while TBP mRNA was used for the internal normalization
S7165	UNC1999 UNC1999一种有效的具有口服活性的EZH2和EZH1选择性抑制剂，无细胞试验中IC50分别为2 nM和45 nM，对广泛表观遗传学相关或不相关的靶点选择性大于1000倍。	Nature, 2018, 560(7718):372-376 Oncogene, 2015, 10.1038/onc.2015.38 J Pathol, 2018, 245(4):433-444	Ex vivo growth of the SCLC PDX LX92 is significantly inhibited by the EZH2 inhibitors EPZ-5687, GSK343 and UNC1999 as measured by resazurin conversion (two-way analysis of variance, adjusted for multiple comparisons by the method of Dunnet).
S7265	MM-102 MM-102是一个高亲和力的多肽模拟的MLL1抑制剂，无细胞试验中IC50为0.4 μM。	Mol Cell Biol, 2015, 36(4):615-27 Biochem Biophys Res Commun, 2016, 469(1):108-13 Cell Physiol Biochem, 2018, 45(4):1529-1540	(D) ChIP-qPCR analysis of the H3K4me3 levels in hESCs synchronized in mitosis with or without MLL1/2 inhibitors. DMSO, cells treated with DMSO only; Noc, cells blocked in mitosis with nocodazole; Noc + MLL Inh, cells blocked in mitosis with nocodazole in the presence of Mi-2 and MM-102 (20 μM each). Values for percent input are normalized to the IgG control (n = 2). One-way analysis of variance followed by Tukey's test for multiple comparisons was performed. , P < 10⁻²; **, P < 10⁻⁵; ns, not significant. (E) Reverse transcription-qPCR analysis of RNA expression levels for bivalent genes after induction of differentiation in unsynchronized H9 ES cells pretreated with MLL inhibitors. Differentiation was induced using E6 medium containing 1 μM RA per 24 h. DMSO, cells pretreated with DMSO only; MLL Inh, cells pretreated with Mi-2 and MM-102 (20 μM each) for 24 h. Unpaired parametric t test with Welch's corrections was performed. Two-tailed P values were calculated. , P < 10⁻²; , P < 10⁻³; *, P < 10⁻⁴; ns, not significant. Log2 RNA levels were normalized against HPRT1 RNA levels and expressed as fold change between undifferentiated and differentiated cells.
S7079	SGC 0946 SGC 0946是一种高效的，选择性的DOT1L甲基转移酶抑制剂，无细胞试验中IC50为0.3 nM，对一系列12 PMTs和DNMT1没有活性。
S3147	Entacapone Entacapone抑制儿茶酚-O-甲基转移酶(COMT)活性，IC50为151 nM。
S8071	UNC0638 UNC0638是一种有效的选择性的组蛋白赖氨酸甲基转移酶（HMTase）抑制剂，作用于G9a和GLP，IC50分别为< 15 nM和19 nM，有效且选择性地作用于多种表观遗传和非表观遗传靶点。
S8607	JQ-EZ-05 (JQEZ5) JQ-EZ-05是可逆的、特异的EZH1/2抑制剂。
S8353	CPI-1205 CPI-1205是具有口服生物活性的选择性组蛋白赖氨酸甲基转移酶EZH2的抑制剂，对EZH2和EZH1的IC50分别为2 nM和52 nM。它具有潜在的抗肿瘤活性。
S7570	UNC0379 UNC0379 是一种选择性，底物竞争性N-lysine methyltransferase SETD8抑制剂，IC50为7.9 μM，选择性比其他15种甲基转移酶高。	Mol Cancer Ther, 2018, 17(7):1585-1594
S7748	EPZ015666(GSK3235025) EPZ015666(GSK3235025) 是一种有效的，选择性且口服生物有效的 PRMT5 抑制剂，K_i 为 5 nM，选择性比其它 PMTs 高 20,000多倍。	J Cell Mol Med, 2017, 21(4):781-790 Cell Signal, 2017, 34:55-65	(B) Effect of EPZ015666 on nuclear translocation of p65. Middle panel showed a representative photo of IF staining of p65 localization (green). Nuclei were stained with DAPI.
S8147	MS049 MS049是有效的、选择性的PRMT4和PRMT6抑制剂，IC50分别为34 nM和43 nM。
S7230	UNC0642 UNC0642是一种有效的、选择性的histone methyltransferases G9a/GLP抑制剂，对G9a和GLP的IC50均小于2.5 nM。对G9a和GLP的选择性比其他激酶、GPCRs、转运体和离子通道高300倍以上。
S8340	SGC2085 SGC2085是一种有效的、选择性的Coactivator Associated Arginine Methyltransferase 1 (CARM1)抑制剂，IC50为50 nM，比对其他PRMTs的选择性高100倍以上。
S7294	PFI-2 HCl PFI-2是一种强效的，有选择性和细胞活性的lysine methyltransferase SETD7抑制剂，K_{i (app)}和IC50分别为0.33 nM 和2 nM，比其他甲基转移酶和非后生的靶点高出1000倍的选择性。
S7983	A-196 A-196是一种有效的、选择性的SUV420H1和SUV420H2抑制剂，IC50s分别为0.025 μM和0.144 μM。选择性比对其他组蛋白转移酶以及非表观遗传靶标高100倍以上。
S4589	Amodiaquine dihydrochloride dihydrate Amodiaquine在人红细胞中是一种有效的、非竞争性的组胺N-甲基转移酶抑制剂，其Ki值为18.6 nM。它也被用作抗疟疾药和消炎药。
S8479	LLY-283 LLY-283是有效的、选择性的SAM竞争性的化学探针，靶向PRMT5。它抑制PRMT5活性，抑制其对H4R3衍生的肽段底物的甲基化，IC50为20 nM。其对PRMT5的选择性比对其他组蛋白甲基转移酶和非表观遗传靶点的选择性高100倍以上。
S7820	EPZ020411 2HCl EPZ020411是有效的、选择性的PRMT6小分子抑制剂，IC50为10 nM。
S7816	MI-463 MI-463是Menin-MLL interaction的有效抑制剂，IC50为15.3 nM。
S7832	SGC707 SGC707是一种有效的，选择性的，且具有细胞活性的蛋白精氨酸甲基转移酶 3 (PRMT3)变构抑制剂，IC50 和 K_d分别为31 nM 和 53 nM。
S7817	MI-503 MI-503是一种有效的、选择性的Menin-MLL抑制剂，IC50为14.7 nM。在人类MLL白血病细胞系中，具有显著的生长抑制效果（GI=250 nM-570 nM），但是在不具有MLL易位的人类白血病细胞中，效果甚微。
S8112	MS023 MS023是一类高效选择性并且有细胞活性的I型PRMT抑制剂，其对PRMT1, PRMT3, PRMT4, PRMT6和PRMT8的IC50分别为30 nM, 119 nM, 83 nM, 4 nM, 和5 nM。
S8068	Chaetocin Chaetocin，一类来自毛壳菌属的天然产物，是一类 histone methyltransferase抑制剂，其对dSU(VAR)3-9，小鼠G9a和粗糙链孢霉 DIM5的IC50分别为0.8 μM, 2.5 μM和3 μM。
S7619	MI-3 (Menin-MLL Inhibitor) MI-3 (Menin-MLL Inhibitor)是一种强效的menin-MLL相互作用抑制剂，IC50为 648 nM。
S7572	A-366 A-366是一种有效的、选择性的G9a/GLP组蛋白甲基转移酶抑制剂，IC50为3.3 nM。对G9a/GLP的选择性比21个其他甲基转移酶高1000倍以上。
S8664	GSK3326595 (EPZ015938) GSK3326595 (EPZ015938)是一种具有口服活性的、有效的、选择性protein arginine methyltransferase 5 (PRMT5)抑制剂，在体内外有效地抑制肿瘤生长。
S7591	BRD4770 BRD4770是一种histone methyltransferase G9a抑制剂，其IC50为6.3 μM，并且会诱导细胞死亡。	Hum Pathol, 2018, 72:117-126
S7805	EPZ011989 EPZ011989是一种有效的、选择性的、具有口服活性的EZH2抑制剂，Ki值<3 nM。	J Cancer, 2018, 9(20):3787-3796
S7618	MI-2 (Menin-MLL Inhibitor) MI-2 (Menin-MLL Inhibitor)是一种有效的menin-MLL相互作用抑制剂，IC50为446 nM。	Mol Cell Biol, 2015, 36(4):615-27
S7575	LLY-507 LLY-507是一种具有细胞活性的和选择性的、有效的蛋白质赖氨酸甲基转移酶SMYD2的抑制剂。
S8111	GSK591 GSK591 (EPZ015866,GSK3203591)是一种有效的、选择性PRMT5抑制剂。	Cancer Med, 2018, 7(3):869-882	Treatment of HCC cells with 500 nmol/L GSK591 for 4 days led to significant loss of PRMT5-catalyzed methylarginine on H4 (H4R3me2s), the upregulation of BTG2, and the phosphorylation of ERK. Inhibition of ERK phosphorylation by PD184352 treatment reversed these effects. H4R3me2s was used to detect the PRMT5 activity. Histone 3 was used as nuclear loading control.
S8209	HLCL-61 HCL HLCL-61 hydrochloride是一种有效的、选择性PRMT5抑制剂，用作治疗急性髓性白血病。
S8494	PF-06726304 PF-06726304是选择性EZH2抑制剂，对WT EZH2和EZH2(Y641N)的Ki值分别为0.7 nM和3 nM。抑制H3K27me3的IC50为15 nM。
S7611	EI1 EI1是一种有效的选择性EZH2抑制剂，对EZH2 (WT)和EZH2 (Y641F)的IC50分别为15 nM和13 nM。	Mol Cancer, 2017, 10.1186/s12943-016-0575-6 Oncotarget, 2015, 6(32):32410-25	EZH2 inhibitors EI1 or GSK343 are applied in MDA-MB-231 breast cancer cells with NBAT1 over-expression. The invasion suppression effects of NBAT1 was reversed by concomitant EZH2 inhibitors.
S8624	JNJ-64619178 JNJ-64619178是PRMT5抑制剂，具有较高的选择性和效力（PRMT5-MEP-50, IC50=0.14 nM）、良好的药代动力学特性以及安全性。
S7804	GSK503 GSK503是一种有效的特异性EZH2甲基转移酶抑制剂。	J Pathol, 2018, 245(4):433-444 Front Immunol, 2016, 7:496	LC3B‐II levels are increased following 120 h treatment of GSK503 (G, CRMM1 and CRMM2 at 10 μm, and CM2005.1 at 15 μm) or UNC1999 (U, 6 μm).
S7353	EPZ004777 EPZ004777是一种有效的，选择性的DOT1L抑制剂，无细胞试验中IC50为0.4 nM。	Theranostics, 2018, 8(16):4359-4371 Int J Cancer, 2017, 141(2):324-335 FEBS J, 2017, 10.1111/febs.14060	THP-1 cells were treated with MI-3 (6.25 μM, 6 days), GSK126 (5 μM, 6 days), or EPZ004777 (5 μM, 6 days), with orwithout PMA (50 ng/mL, 12 h), and surface expression of CD11b was determined by ﬂow cytometric analysis. The data are representedas the mean ± SD, n = 3. THP-1 cells were collected for Wright-Giemsa staining.
S7061	GSK126 GSK126 是一种有效的，高选择性EZH2 methyltransferase抑制剂，IC50为9.9 nM，对 EZH2 的选择性比其他20种人甲基转移酶高1000多倍。	Nature, 2019, 566(7743):270-274 Nature, 2019, 566(7744):344-349 Mol Cancer, 2017, 16(1):22	HeLa cells were transfected with NS (nonspecific) or EZH2-specific siRNA for 48 h with protease inhibitors (10 μM E64 and 10 μM pepstatin-A). Cells were stained with LC3B antibody (green) and DAPI, and observed under confocal microscopy for LC3B puncta. Scale bars: 10 μm
S7656	CPI-360 CPI-360是一种有效的，选择性的，且SAM竞争性EZH1抑制剂，IC50为102.3 nM，选择性比作用于其它甲基转移酶高100多倍。
S7616	CPI-169 CPI-169是一种有效的选择性EZH2抑制剂，作用于EZH2 WT，EZH2 Y641N，和EZH1的IC50分别为0.24 nM，0.51 nM，和6.1 nM。
S7884	AMI-1 AMI-1是一种有效的特异性Histone Methyltransferase (HMT)抑制剂，对酵母 Hmt1p 和人 PRMT1 的IC50分别为 3.0 μM 和 8.8 μM。	Nitric Oxide, 2017, 67:58-67	Effects of microinjection of AMI-1 into the RVLM on cardiovascular activity in the Ang II-induced hypertensive rats. The representative original tracings (A)
S7815	MI-136 MI-136抑制DHT所诱导的雄激素受体(AR)靶向基因的表达。

产品目录	产品描述	文献引用	实验数据
S7833	OICR-9429 OICR-9429是一种有效的WDR5-MLL、WDR5-Histone3相互作用的拮抗剂，能在体外实验中降低急性髓性白血病细胞的活性。它与WDR5高亲和结合，Kd值为93 ± 28 nM。	Theranostics, 2018, 8(18):5143-5158	(F) Real-time PCR analysis showed the VEGFA mRNA expression in the HOXC10-overexpressing glioma cells treated with vehicle or 1 μM OICR-9429 for 2 days. (G) ChIP-qPCR enrichments of H3K4me3, polymerase II or IgG on VEGFA promoter region 3 in the HOXC10-overexpressing glioma cells treated with vehicle or 1 μM OICR-9429 for 2 days. All the assays shown in the figure were independently replicated three times. Error bars, SD. * P < 0.05.
S8359	UNC3866 UNC3866是染色质域的多梳蛋白家族CBX和CDY的甲基赖氨酸阅读功能拮抗剂。它与CBX4和CBX7的染色质域有效结合，Kd值约为100 nM, 对CBX4和CBX7的选择性分别是对其他CBX和CDY染色质域的6倍和18倍。

产品目录

产品描述

文献引用

实验数据

S7833