Histone Demethylase
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 | ||
| S7070 | GSK J4 HCl | 90 mg/mL | 90 mg/mL | 90 mg/mL |
| S7237 | OG-L002 | <1 mg/mL | 45 mg/mL | 19 mg/mL |
| S7281 | JIB-04 | <1 mg/mL | 25 mg/mL | <1 mg/mL |
| S7296 | ML324 | <1 mg/mL | 43 mg/mL | 3 mg/mL |
| S8287 | CPI-455 HCl | <1 mg/mL | 10 mg/mL | 2 mg/mL |
| S4800 | Daminozide | -1 mg/mL | ||
| S7574 | GSK-LSD1 2HCl | 57 mg/mL | 57 mg/mL | -1 mg/mL |
| S7234 | IOX1 | <1 mg/mL | 37 mg/mL | <1 mg/mL |
| S7795 | ORY-1001 (RG-6016) 2HCl | 61 mg/mL | 5 mg/mL | 4 mg/mL |
| S7581 | GSK J1 | <1 mg/mL | 77 mg/mL | <1 mg/mL |
| S7796 | GSK2879552 2HCl | 44 mg/mL | 29 mg/mL | <1 mg/mL |
| S7680 | SP2509 | <1 mg/mL | 38 mg/mL | <1 mg/mL |
| S8601 | CP2 | 100 mg/mL | -1 mg/mL | -1 mg/mL |
- Histone Demethylase抑制剂（13）
- 新Histone Demethylase产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7070 |
GSK J4 HClGSK J4 HCl是一种细胞渗透性的GSK J1前体药物，是第一个选择性H3K27组蛋白去甲基化酶JMJD3和UTX抑制剂，无细胞试验中IC50为60 nM，抑制JMJ家族的去甲基化酶活性。 |
DIPG cells were seeded into 96-well plates and treated with panobinostat and GSK-J4 individually or in combination at the indicated concentrations for 72 hr in at least triplicate. Cell viabilities were then assessed using the CelltiterGlo assay relative to 0.1% DMSO control. Data shown as mean ± SD. *indicates the two drugs demonstrate synergy at that condition (i.e. CI < 1). |
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| S7237 |
OG-L002OG-L002是一种有效的，特异性LSD1抑制剂，无细胞试验中IC50为20 nM，比作用于MAO-B和MAO-A选择性分别高36和69倍。 |
Effect of treatment on equine herpesvirus type 1 (EHV-1) viral load during lytic infection of primary equine fetal kidney cells. At 24 hpi, reduced EHV-1 DNA copies per cell were detected in the presence of ganciclovir (**p = 0.0005) or OG-L002 (*p = 0.005), and markedly when both treatments (***p < 0.0001) were applied simultaneously in comparison with DMSO control vehicle. Combined treatment decreased the number of EHV-1 DNA copies in comparison to treatment with ganciclovir alone (p = 0.01) or OG-L002 alone (p = 0.001). Lines represent mean values.
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| S7281 |
JIB-04JIB-04是一种广谱的选择性Jumonji histone demethylase抑制剂，无细胞试验中对JARID1A，JMJD2E，JMJD3，JMJD2A，JMJD2B，JMJD2C和JMJD2D的IC50分别是230 nM，340 nM，855 nM，445 nM，435 nM，1100 nM和290 nM。 |
G, Western blot analyses to monitor the amount of H3K9me3 in the presence of rhein and MMS (upper panel) and under the
treatment of JIB-04 (lower panel).
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| S7296 |
ML324ML324是一种选择性的jumonji histone demethylase (JMJD2)抑制剂， 其对JMJD2E的IC50为920 nM。 |
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| S8287 |
CPI-455 HClCPI-455是特异性KDM5抑制剂，抑制全长KDM5A的IC50值为10 nM。在多种癌细胞系的治疗中，结合标准化疗或者靶向制剂，CPI-455能提高H3K4三甲基化（H3K4me3）整体水平，并减少DTPs的数量。 |
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| S4800New |
DaminozideDaminozide, a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily with IC50 of 1.5±0.7 μM for KDM2A. It is at least 100-fold selective as an inhibitor of the KDM2/7 subfamily over the other demethylase subfamily members tested, with IC50s of 2 μM or less against KDM2A, PHF8, and KIAA1718 and IC50s of 127 μM for KDM3A or greater (mM range) against other demethylases. |
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| S7574 |
GSK-LSD1 2HClGSK-LSD1 2HCl是一种不可逆的选择性 LSD1抑制剂，IC50 为 16 nM，选择性比其它密切相关的FAD可利用酶(即 LSD2，MAO-A，MAO-B)高1000多倍。 |
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| S7234 |
IOX1IOX1 是2OG oxygenases强效的广谱抑制剂, 包括JmjC demethylases。 |
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| S7795 |
ORY-1001 (RG-6016) 2HClORY-1001 (RG-6016) 2HCl是一种口服具有活性的，选择性的，赖氨酸特异性脱甲基酶LSD1/KDM1A抑制剂，IC50为<20 nM，对相关的FAD依赖性氨基氧化酶具有高度选择性。Phase 1。 |
Cells were exposed to drugs for 48 h or for the indicated times. Cell death and Dwm dissipation were determined by flow cytometric analyses of propidium iodide uptake or DiOC6(3) staining, respectively. Caspase 3/7 activity was determined using the fluorogenic substrate Ac-DEVD-AMC; relative caspase 3/7 activities are the ratio of treated cells to untreated cells.
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| S7581 |
GSK J1GSK-J1是一种高效的 H3K27 histone demethylase 抑制剂，无细胞试验中对JMJD3 (KDM6B) 和 UTX (KDM6A)的 IC50 分别为 28 nM 和 53 nM，比作用于其他测试的脱甲基酶选择性高10倍多。 |
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| S7796 |
GSK2879552 2HClGSK2879552 2HCl 是一种有效的、选择性的、具有生物口服活性的、不可逆的LSD1的抑制剂，Kiapp=1.7 μM。 |
Effects of LSD1 inhibitors in acute myeloid leukaemia cells. Cells were exposed to drugs for 48 h or for the indicated times. Cell death and Dwm dissipation were determined by flow cytometric analyses of propidium iodide uptake or DiOC6(3) staining, respectively. Caspase 3/7 activity was determined using the fluorogenic substrate Ac-DEVD-AMC; relative caspase 3/7 activities are the ratio of treated cells to untreated cells. Means±SEM of each two (caspase 3/7 activity) or three (flow cytometric analyses) separate measurements are shown.
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| S7680 |
SP2509SP2509是一种选择性histone demethylase LSD1抑制剂，IC50为 13 nM，对MAO-A，MAO-B，乳酸脱氢酶和葡萄糖氧化酶没有活性。 |
Cells were exposed to drugs for 48 h or for the indicated times. Cell death and Dwm dissipation were determined by flow cytometric analyses of propidium iodide uptake or DiOC6(3) staining, respectively. Caspase 3/7 activity was determined using the fluorogenic substrate Ac-DEVD-AMC; relative caspase 3/7 activities are the ratio of treated cells to untreated cells.
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| S8601 |
CP2CP2是一种环肽，能够抑制JmjC histone demethylases KDM4，对KDM4A和KDM4C的IC50分别为42 nM和29 nM。 |
