Histone Methyltransferase
信号通路图
研究领域
抑制剂选择性比较
Histone Methyltransferase产品
| 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Ki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。 |
Treatment of c-Kit+ bone marrow (BM) cells from Setd2f/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 |
EPZ005687EPZ005687是一种有效的，选择性EZH2抑制剂，无细胞试验中Ki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。 |
Western blot analysis of day 7 lysates from LX92 lysates treated with various EZH2 inhibitors. |
|
| S7164 |
GSK343GSK343 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。GSK343 可诱导自噬。 |
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 01294BIX01294 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。BIX01294 可诱导自噬。BIX01294 还可通过癌蛋白 NSD1、NSD2 和 NSD3 来抑制H3K36甲基化。 |
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, E7438)是一种有效的，选择性EZH2抑制剂，无细胞试验中Ki 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。 |
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.
|
|
| S7820New |
EPZ020411 2HClEPZ020411是有效的、选择性的PRMT6小分子抑制剂，IC50为10 nM。 |
||
| S7120 |
3-deazaneplanocin A (DZNeP) HCl3-deazaneplanocin A HCl (DZNeP, NSC 617989)，一种腺苷类似物，是竞争性S-adenosylhomocysteine hydrolase抑制剂，无细胞试验中Ki为50 pM。 |
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 |
UNC1999UNC1999 是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。UNC1999 是一种有效的 autophagy 自噬诱导剂。UNC1999 可特异性地抑制H3K27me3/2并诱导一系列抗白血病作用，包括抗增殖、分化和细胞凋亡。 |
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-102MM-102 (HMTase Inhibitor IX)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。 |
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 0946SGC 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 |
EntacaponeEntacapone (OR-611) 抑制儿茶酚-O-甲基转移酶(COMT)活性，IC50为151 nM。Entacapone 是一种 FTO demethylation 的抑制剂，IC50为3.5 μM，可用于代谢紊乱的研究。 |
||
| S8071 |
UNC0638UNC0638 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。UNC0638 具有抗病毒的活性。 |
||
| S8607 |
JQ-EZ-05 (JQEZ5)JQ-EZ-05 (JQEZ5) 是可逆的、特异的EZH1/2抑制剂。 |
||
| S8353 |
Lirametostat (CPI-1205)Lirametostat (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。 |
||
| S7020 |
UNC0646UNC0646是一种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6 nM和15 nM 。在多种细胞系中活性较强，也能有效的将功能性活性于细胞毒性区分。 |
||
| S4021 |
TolcaponeTolcapone (Ro 40-7592) 是一种有效和选择性的可逆硝基酚类儿茶酚-O-甲基转移酶(COMT)抑制剂，Ki为30nM。 |
||
| S7570 |
UNC0379UNC0379 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。 |
||
| 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，Ki 为 5 nM，选择性比其它 PMTs 高 20,000多倍。 |
(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 |
MS049MS049是有效的、选择性的PRMT4和PRMT6抑制剂，IC50分别为34 nM和43 nM。 |
||
| S7230 |
UNC0642UNC0642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 |
SGC2085SGC2085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 HClPFI-2是一种强效的，有选择性和细胞活性的lysine methyltransferase SETD7抑制剂，Ki (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-196A-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 dihydrateAmodiaquine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。 |
||
| S7816 |
MI-463MI-463是Menin-MLL interaction的有效抑制剂，IC50为15.3 nM。 |
||
| S7868 |
S-Adenosyl-L-homocysteine (SAH)S-Adenosyl-L-homocysteine (SAH, S-Adenosylhomocysteine, AdoHcy, Formycinylhomocysteine) 是一种 (Methyltransferase Like 3-14) METTL3-METTL14 heterodimer complex (METTL3-14) 的抑制剂，其IC50值为0.9 μM。 |
||
| S7832 |
SGC707SGC707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 Kd分别为31 nM 和 53 nM。 |
||
| S7817 |
MI-503MI-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 |
MS023MS023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 |
ChaetocinChaetocin，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。Chaetocin是一种抗癌药物并是 thioredoxin reductase (TrxR) 的抑制剂。 |
||
| 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。 |
||
| S7572 |
A-366A-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 |
Pemrametostat (GSK3326595)Pemrametostat (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 |
BRD4770BRD4770是一种histone methyltransferase G9a抑制剂，其IC50为6.3 μM，并且会诱导细胞死亡。 |
||
| S8918 |
MS1943MS1943 是一种口服可生物利用的 EZH2 的选择性降解剂，可有效降低细胞中的EZH2水平，其抑制EZH2甲基转移酶活性的IC50值为120 nM。 |
||
| S7805 |
EPZ011989EPZ011989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。 |
||
| S8702 |
EBI-2511EBI-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。 |
||
| S8934 |
VTP50469VTP50469 是一种有效的、高选择性和口服活性的 Menin-MLL interaction 的抑制剂，Ki值为104 pM。VTP50469 具有抗白血病的活性。 |
||
| 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。 |
||
| S7575 |
LLY-507LLY-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 |
GSK591GSK591 (EPZ015866, GSK3203591)是一种有效的、选择性PRMT5抑制剂。 |
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 HCLHLCL-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。 |
||
| S9659 |
UNC6852UNC6852 是一种选择性降解剂靶向 polycomb repressive complex 2 (PRC2)，对EED的IC50值为247 nM。UNC6852 的结构基于PROTAC，包含一个EED226衍生的配体和一个VHL的配体。 |
||
| S8983 |
MAK683MAK683 (EED inhibitor-1, example 2) 是一种 embryonic ectoderm development (EED) 的抑制剂。MAK683 在EED Alphascreen binding、LC-MS和ELISA分析中对应的IC50值分别为59 nM、89 nM和26 nM。 |
||
| S8494 |
PF-06726304PF-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 |
EI1EI1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。 |
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 |
Onametostat (JNJ-64619178)Onametostat (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 |
GSK503GSK503是一种有效的特异性EZH2甲基转移酶抑制剂。 |
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 |
EPZ004777EPZ004777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。 |
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 |
GSK126GSK126 (GSK2816126A, GSK2816126) 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。 |
(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-360CPI-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-169CPI-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-1AMI-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。 |
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-136MI-136抑制DHT所诱导的雄激素受体(AR)靶向基因的表达。 |
||
| S7833 |
OICR-9429OICR-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。 |
(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 |
UNC3866UNC3866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。 |
||
| S2184 |
WDR5-0103WDR5-0103 (WD-Repeat Protein 5-0103)是一种WDR5 (WD40 repeat protein 5)的小分子拮抗剂，Kd值为450 nM。 |
||
| S8496 |
EED226EED226是一种有效的、选择性的、具有口服活性的Polycomb repressive complex 2 (PRC2)抑制剂，以H3K27me0 peptide为底物时，IC50=23.4 nM; 以单核小体为底物时，IC50=53.5 nM。它与EED的H3K27me3结合口袋直接相互作用。 |
| 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Ki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。 |
Treatment of c-Kit+ bone marrow (BM) cells from Setd2f/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 |
EPZ005687EPZ005687是一种有效的，选择性EZH2抑制剂，无细胞试验中Ki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。 |
Western blot analysis of day 7 lysates from LX92 lysates treated with various EZH2 inhibitors. |
|
| S7164 |
GSK343GSK343 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。GSK343 可诱导自噬。 |
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 01294BIX01294 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。BIX01294 可诱导自噬。BIX01294 还可通过癌蛋白 NSD1、NSD2 和 NSD3 来抑制H3K36甲基化。 |
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, E7438)是一种有效的，选择性EZH2抑制剂，无细胞试验中Ki 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。 |
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.
|
|
| S7820New |
EPZ020411 2HClEPZ020411是有效的、选择性的PRMT6小分子抑制剂，IC50为10 nM。 |
||
| S7120 |
3-deazaneplanocin A (DZNeP) HCl3-deazaneplanocin A HCl (DZNeP, NSC 617989)，一种腺苷类似物，是竞争性S-adenosylhomocysteine hydrolase抑制剂，无细胞试验中Ki为50 pM。 |
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 |
UNC1999UNC1999 是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。UNC1999 是一种有效的 autophagy 自噬诱导剂。UNC1999 可特异性地抑制H3K27me3/2并诱导一系列抗白血病作用，包括抗增殖、分化和细胞凋亡。 |
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-102MM-102 (HMTase Inhibitor IX)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。 |
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 0946SGC 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 |
EntacaponeEntacapone (OR-611) 抑制儿茶酚-O-甲基转移酶(COMT)活性，IC50为151 nM。Entacapone 是一种 FTO demethylation 的抑制剂，IC50为3.5 μM，可用于代谢紊乱的研究。 |
||
| S8071 |
UNC0638UNC0638 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。UNC0638 具有抗病毒的活性。 |
||
| S8607 |
JQ-EZ-05 (JQEZ5)JQ-EZ-05 (JQEZ5) 是可逆的、特异的EZH1/2抑制剂。 |
||
| S8353 |
Lirametostat (CPI-1205)Lirametostat (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。 |
||
| S7020 |
UNC0646UNC0646是一种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6 nM和15 nM 。在多种细胞系中活性较强，也能有效的将功能性活性于细胞毒性区分。 |
||
| S4021 |
TolcaponeTolcapone (Ro 40-7592) 是一种有效和选择性的可逆硝基酚类儿茶酚-O-甲基转移酶(COMT)抑制剂，Ki为30nM。 |
||
| S7570 |
UNC0379UNC0379 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。 |
||
| 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，Ki 为 5 nM，选择性比其它 PMTs 高 20,000多倍。 |
(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 |
MS049MS049是有效的、选择性的PRMT4和PRMT6抑制剂，IC50分别为34 nM和43 nM。 |
||
| S7230 |
UNC0642UNC0642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 |
SGC2085SGC2085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 HClPFI-2是一种强效的，有选择性和细胞活性的lysine methyltransferase SETD7抑制剂，Ki (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-196A-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 dihydrateAmodiaquine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。 |
||
| S7816 |
MI-463MI-463是Menin-MLL interaction的有效抑制剂，IC50为15.3 nM。 |
||
| S7868 |
S-Adenosyl-L-homocysteine (SAH)S-Adenosyl-L-homocysteine (SAH, S-Adenosylhomocysteine, AdoHcy, Formycinylhomocysteine) 是一种 (Methyltransferase Like 3-14) METTL3-METTL14 heterodimer complex (METTL3-14) 的抑制剂，其IC50值为0.9 μM。 |
||
| S7832 |
SGC707SGC707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 Kd分别为31 nM 和 53 nM。 |
||
| S7817 |
MI-503MI-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 |
MS023MS023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 |
ChaetocinChaetocin，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。Chaetocin是一种抗癌药物并是 thioredoxin reductase (TrxR) 的抑制剂。 |
||
| 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。 |
||
| S7572 |
A-366A-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 |
Pemrametostat (GSK3326595)Pemrametostat (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 |
BRD4770BRD4770是一种histone methyltransferase G9a抑制剂，其IC50为6.3 μM，并且会诱导细胞死亡。 |
||
| S8918 |
MS1943MS1943 是一种口服可生物利用的 EZH2 的选择性降解剂，可有效降低细胞中的EZH2水平，其抑制EZH2甲基转移酶活性的IC50值为120 nM。 |
||
| S7805 |
EPZ011989EPZ011989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。 |
||
| S8702 |
EBI-2511EBI-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。 |
||
| S8934 |
VTP50469VTP50469 是一种有效的、高选择性和口服活性的 Menin-MLL interaction 的抑制剂，Ki值为104 pM。VTP50469 具有抗白血病的活性。 |
||
| 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。 |
||
| S7575 |
LLY-507LLY-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 |
GSK591GSK591 (EPZ015866, GSK3203591)是一种有效的、选择性PRMT5抑制剂。 |
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 HCLHLCL-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。 |
||
| S9659 |
UNC6852UNC6852 是一种选择性降解剂靶向 polycomb repressive complex 2 (PRC2)，对EED的IC50值为247 nM。UNC6852 的结构基于PROTAC，包含一个EED226衍生的配体和一个VHL的配体。 |
||
| S8983 |
MAK683MAK683 (EED inhibitor-1, example 2) 是一种 embryonic ectoderm development (EED) 的抑制剂。MAK683 在EED Alphascreen binding、LC-MS和ELISA分析中对应的IC50值分别为59 nM、89 nM和26 nM。 |
||
| S8494 |
PF-06726304PF-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 |
EI1EI1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。 |
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 |
Onametostat (JNJ-64619178)Onametostat (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 |
GSK503GSK503是一种有效的特异性EZH2甲基转移酶抑制剂。 |
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 |
EPZ004777EPZ004777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。 |
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 |
GSK126GSK126 (GSK2816126A, GSK2816126) 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。 |
(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-360CPI-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-169CPI-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-1AMI-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。 |
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-136MI-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-9429OICR-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。 |
(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 |
UNC3866UNC3866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。 |
||
| S2184 |
WDR5-0103WDR5-0103 (WD-Repeat Protein 5-0103)是一种WDR5 (WD40 repeat protein 5)的小分子拮抗剂，Kd值为450 nM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S8496 |
EED226EED226是一种有效的、选择性的、具有口服活性的Polycomb repressive complex 2 (PRC2)抑制剂，以H3K27me0 peptide为底物时，IC50=23.4 nM; 以单核小体为底物时，IC50=53.5 nM。它与EED的H3K27me3结合口袋直接相互作用。 |
沪公网安备 31011502012800号