Histone Methyltransferase

信号通路图

研究领域

抑制剂选择性比较

Histone Methyltransferase产品

所有产品 Histone Methyltransferase抑制剂(48) Histone Methyltransferase拮抗剂(2)

目录号	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。	Sci Adv, 2019, 5(2):eaav5590 EMBO J, 2019, 38(14):e101564 Cell Rep, 2019, 27(3):971-986	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。	Cell Rep, 2019, 27(11):3331-3344 Int J Cancer, 2019, 145(2):415-426 Mol Oncol, 2019, 13(7):1589-1604	Western blot analysis of day 7 lysates from LX92 lysates treated with various EZH2 inhibitors.
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。	Nat Commun, 2019, 10(1):2427 J Immunother Cancer, 2019, 7(1):277 Cancer Res, 2019, 79(10):2761-2774	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 Cell, 2019, 35(5):752-766 Sci Adv, 2019, 5(3):eaau7566 Nucleic Acids Res, 2019, 47(5):2349-2364	The H3K9me2 inhibitor BIX01294 mimics the effects of BPA and DEHP on the expression of meiotic genes and Plzf in cultured testes. (A) representative double IF staining for Mvh (green) and Stra8 (red) and Scp3 (red) and (B) Plzf (red) in histological sections of control and BIX01294-treated testes. (C) RT-qPCR analysis of Stra8, Scp3, Rec8, Spo11 and plzf in testes from the control and BIX01294-treated groups. Data are represented as the mean ± SEM. ns, P > 0.05, P < 0.05; *P < 0.01.
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。	Clin Cancer Res, 2020, 26(1):290-300 Cancer Cell, 2019, 36(5):512-527 Nat Commun, 2019, 10(1):5114	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.
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。	Cancer Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 35(6):885-900	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。	Br J Pharmacol, 2019, 10.1111/bph.14754 Epigenetics, 2019, 1-16 Oncol Lett, 2019, 18(1):907-915	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。	Dev Cell, 2019, 49(6):867-881 Cell Oncol (Dordr), 2019, 42(4):505-520 Cell Physiol Biochem, 2018, 45(4):1529-1540	Immunofluorescence staining of H3K4me2/3 (red) in the IVF, SCNT and MM-102-NT embryos. The nuclei (blue) were stained with DAPI. The merged images of H3K4me2/3 and DNA were purple. Scale bars: 50 μm.
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。	Cancer Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193 Sci Adv, 2019, 5(2):eaav5590
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。	Clin Epigenetics, 2019, 11(1):165 Biochim Biophys Acta Gene Regul Mech, 2019, 1862(2):173-183
S8607	JQ-EZ-05 (JQEZ5) JQ-EZ-05是可逆的、特异的EZH1/2抑制剂。	Nat Chem Biol, 2019, 15(4):391-400
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。	Clin Cancer Res, 2019, 10.1158/1078-0432
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。	Biochim Biophys Acta Gene Regul Mech, 2019, 1862(2):173-183 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。	Theranostics, 2019, 9(9):2606-2617 EBioMedicine, 2019, 44:98-111 Front Immunol, 2019, 10:174	(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。	Clin Epigenetics, 2019, 11(1):165
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。	Nucleic Acids Res, 2019, 47(21):10977-10993 J Immunother Cancer, 2019, 7(1):277
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。
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。	J Immunother Cancer, 2019, 7(1):277
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。	Nat Commun, 2019, 10(1):273 Cell Death Dis, 2019, 10(12):894 Arch Biochem Biophys, 2019, 10.1016/j.abb.2019.06.010
S5445	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.
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。	Clin Epigenetics, 2019, 11(1):137
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。	Nat Med, 2019, 25(7):1073-1081
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。	Oncogene, 2019, 38(46):7181-7195 Cancer Med, 2019, 8(5):2414-2428
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。	Cancer Cell, 2019, 36(4):385-401 J Cancer, 2018, 9(20):3787-3796
S8702	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。
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。	Cell Rep, 2019, 26(2):415-428 Endocrinology, 2019, 10.1210/en.2019-00274 Front Oncol, 2018, 8:632
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。	J Immunother Cancer, 2019, 7(1):277
S8111	GSK591 GSK591 (EPZ015866,GSK3203591)是一种有效的、选择性PRMT5抑制剂。	J Immunother Cancer, 2019, 7(1):277 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。	Nat Commun, 2018, 9(1):1572
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 Virology, 2017, 506:34-44 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。	Cancer Cell, 2019, 36(4):385-401 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。	Cancer Cell, 2019, 35(5):752-766 Sci Adv, 2019, 5(2):eaav5590 Cancers (Basel), 2019, 11(11)	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。	Exp Cell Res, 2020, 386(2):111743 Nature, 2019, 566(7743):270-274 Nature, 2019, 566(7744):344-349	(C) Four GCBDLBCL cells lines [1 wild-type (wt), 3 mutated (mut) EZH2] were treated with 500 nmol/l BAY 1238097 or with an EZH2 inhibitor (DZNep and GSK126, both used at the concentration of 500 nmol/l) as single agents and in combination for 72 h. The arrow indicates the EZH2 correct band. Dimethyl sulphoxide (DMSO) alone was added as negative control cells. Membranes were hybridized with antibodies against EZH2, H3K27me3, histone H3 and GAPDH.
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。	Nat Commun, 2018, 9(1):4116 Virology, 2017, 506:34-44
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。

目录号	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。	Sci Adv,2019, 5(2):eaav5590 EMBO J,2019, 38(14):e101564 Cell Rep,2019, 27(3):971-986	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。	Cell Rep,2019, 27(11):3331-3344 Int J Cancer,2019, 145(2):415-426 Mol Oncol,2019, 13(7):1589-1604	Western blot analysis of day 7 lysates from LX92 lysates treated with various EZH2 inhibitors.
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。	Nat Commun,2019, 10(1):2427 J Immunother Cancer,2019, 7(1):277 Cancer Res,2019, 79(10):2761-2774	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 Cell,2019, 35(5):752-766 Sci Adv,2019, 5(3):eaau7566 Nucleic Acids Res,2019, 47(5):2349-2364	The H3K9me2 inhibitor BIX01294 mimics the effects of BPA and DEHP on the expression of meiotic genes and Plzf in cultured testes. (A) representative double IF staining for Mvh (green) and Stra8 (red) and Scp3 (red) and (B) Plzf (red) in histological sections of control and BIX01294-treated testes. (C) RT-qPCR analysis of Stra8, Scp3, Rec8, Spo11 and plzf in testes from the control and BIX01294-treated groups. Data are represented as the mean ± SEM. ns, P > 0.05, P < 0.05; *P < 0.01.
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。	Clin Cancer Res,2020, 26(1):290-300 Cancer Cell,2019, 36(5):512-527 Nat Commun,2019, 10(1):5114	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.
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。	Cancer Cell,2019, 36(2):179-193 Cell,2019, 36(2):179-193 Cancer Cell,2019, 35(6):885-900	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。	Br J Pharmacol,2019, 10.1111/bph.14754 Epigenetics,2019, 1-16 Oncol Lett,2019, 18(1):907-915	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。	Dev Cell,2019, 49(6):867-881 Cell Oncol (Dordr),2019, 42(4):505-520 Cell Physiol Biochem,2018, 45(4):1529-1540	Immunofluorescence staining of H3K4me2/3 (red) in the IVF, SCNT and MM-102-NT embryos. The nuclei (blue) were stained with DAPI. The merged images of H3K4me2/3 and DNA were purple. Scale bars: 50 μm.
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。	Cancer Cell,2019, 36(2):179-193 Cell,2019, 36(2):179-193 Sci Adv,2019, 5(2):eaav5590
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。	Clin Epigenetics,2019, 11(1):165 Biochim Biophys Acta Gene Regul Mech,2019, 1862(2):173-183
S8607	JQ-EZ-05 (JQEZ5) JQ-EZ-05是可逆的、特异的EZH1/2抑制剂。	Nat Chem Biol,2019, 15(4):391-400
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。	Clin Cancer Res,2019, 10.1158/1078-0432
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。	Biochim Biophys Acta Gene Regul Mech,2019, 1862(2):173-183 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。	Theranostics,2019, 9(9):2606-2617 EBioMedicine,2019, 44:98-111 Front Immunol,2019, 10:174	(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。	Clin Epigenetics,2019, 11(1):165
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。	Nucleic Acids Res,2019, 47(21):10977-10993 J Immunother Cancer,2019, 7(1):277
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。
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。	J Immunother Cancer,2019, 7(1):277
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。	Nat Commun,2019, 10(1):273 Cell Death Dis,2019, 10(12):894 Arch Biochem Biophys,2019, 10.1016/j.abb.2019.06.010
S5445	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.
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。	Clin Epigenetics,2019, 11(1):137
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。	Nat Med,2019, 25(7):1073-1081
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。	Oncogene,2019, 38(46):7181-7195 Cancer Med,2019, 8(5):2414-2428
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。	Cancer Cell,2019, 36(4):385-401 J Cancer,2018, 9(20):3787-3796
S8702	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。
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。	Cell Rep,2019, 26(2):415-428 Endocrinology,2019, 10.1210/en.2019-00274 Front Oncol,2018, 8:632
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。	J Immunother Cancer,2019, 7(1):277
S8111	GSK591 GSK591 (EPZ015866,GSK3203591)是一种有效的、选择性PRMT5抑制剂。	J Immunother Cancer,2019, 7(1):277 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。	Nat Commun,2018, 9(1):1572
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 Virology,2017, 506:34-44 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。	Cancer Cell,2019, 36(4):385-401 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。	Cancer Cell,2019, 35(5):752-766 Sci Adv,2019, 5(2):eaav5590 Cancers (Basel),2019, 11(11)	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。	Exp Cell Res,2020, 386(2):111743 Nature,2019, 566(7743):270-274 Nature,2019, 566(7744):344-349	(C) Four GCBDLBCL cells lines [1 wild-type (wt), 3 mutated (mut) EZH2] were treated with 500 nmol/l BAY 1238097 or with an EZH2 inhibitor (DZNep and GSK126, both used at the concentration of 500 nmol/l) as single agents and in combination for 72 h. The arrow indicates the EZH2 correct band. Dimethyl sulphoxide (DMSO) alone was added as negative control cells. Membranes were hybridized with antibodies against EZH2, H3K27me3, histone H3 and GAPDH.
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。	Nat Commun,2018, 9(1):4116 Virology,2017, 506:34-44
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。

目录号	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。

目录号

产品描述

文献引用

实验数据

S7833