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) | ||
|---|---|---|---|---|
| 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 |
| S5445 | AMI-1, free acid | -1 mg/mL | 20 mg/mL | -1 mg/mL |
| S7230 | UNC0642 | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S8479 | LLY-283 | <1 mg/mL | 68 mg/mL | 68 mg/mL |
| S8071 | UNC0638 | 6 mg/mL | 100 mg/mL | 100 mg/mL |
| S8664 | GSK3326595 (EPZ015938) | <1 mg/mL | 90 mg/mL | 90 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 |
| 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 |
| 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 |
| 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 |
| 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抑制剂（50）
- 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。 |
Western blot validation of H3K79me2 depletion in Jurkat cells. Mixtures of 0%–100% EPZ5676-treated cells (0:100; 25:75; 50:50, 75:25; 100:0 proportions of [DMSO-treated:EPZ5676-treated] cells) were measured by immunoblot (IB) for the presence of H3K79me2, H3K4me3, or total histone H3 (loading control). Treated cells were exposed to 20 μM EPZ5676 for 4 days.
|
|
| 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。 |
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。 |
(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。 |
we examined the E-cadherin, ZEB1 and Snail expressions after using EZH2 RNAi, DZNeP and EPZ-6438. “*”represent P<0.05 when compared with control group.
|
|
| S5445New |
AMI-1, free acidAMI-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. |
||
| S8607New |
JQ-EZ-05 (JQEZ5)JQ-EZ-05是可逆的、特异的EZH1/2抑制剂。 |
||
| S7230New |
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。 |
||
| S8479New |
LLY-283LLY-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。 |
||
| S8071New |
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。 |
||
| S8664New |
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。 |
||
| S7120 |
3-deazaneplanocin A (DZNeP) HCl3-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。 |
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。 |
(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 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抑制儿茶酚-O-甲基转移酶(COMT)活性，IC50为151 nM。 |
||
| S8353 |
CPI-1205CPI-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 |
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。 |
||
| 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。 |
||
| S7820 |
EPZ020411 2HClEPZ020411是有效的、选择性的PRMT6小分子抑制剂，IC50为10 nM。 |
||
| S7816 |
MI-463MI-463是Menin-MLL interaction的有效抑制剂，IC50为15.3 nM。 |
||
| 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。 |
||
| 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。 |
||
| 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。 |
||
| 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。 |
||
| 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。 |
||
| 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 |
JNJ-64619178JNJ-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。 |
||
| 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 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。 |
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-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。 |
||
| 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。 |
