ヒストン脱メチル化酵素 (Histone Demethylase)
シグナル伝達経路
研究分野
- 阻害剤の選択性比較
- 溶解度
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| 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 |
| S7574 | GSK-LSD1 2HCl | 57 mg/mL | 57 mg/mL | -1 mg/mL |
| S5772 | AS-8351 | <1 mg/mL | 58 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 |
| S4800 | Daminozide | -1 mg/mL | 32 mg/mL | -1 mg/mL |
Histone Demethylase製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S7070 |
GSK J4 HClGSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family. |
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). |
|
| S7237 |
OG-L002OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM in a cell-free assay, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively. |
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.
|
|
| S7281 |
JIB-04JIB-04 is a pan-selective Jumonji histone demethylase inhibitor with IC50 of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D in cell-free assays, respectively. |
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).
|
|
| S7296 |
ML324ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM. |
||
| S7574 |
GSK-LSD1 2HClGSK-LSD1 2HCl is an irreversible, and selective LSD1 inhibitor with IC50 of 16 nM, > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B). |
||
| S5772新 |
AS-8351AS-8351 is a histone demethylase inhibitor that could induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes. |
||
| S7234 |
IOX1IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. |
||
| S7795 |
ORY-1001 (RG-6016) 2HClORY-1001 (RG-6016) 2HCl is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor with IC50 of <20 nM, with high selectivity against related FAD dependent aminoxidases. 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.
|
|
| S7581 |
GSK J1GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, >10-fold selectivity over other tested demethylases. |
||
| S7796 |
GSK2879552 2HClGSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1. |
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.
|
|
| S7680 |
SP2509SP2509 is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. |
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.
|
|
| S8601 |
CP2CP2 is a cyclic peptide that inhibits the JmjC histone demethylases KDM4 with IC50 values of 42 nM and 29 nM for KDM4A and KDM4C, respectively. |
||
| S4800 |
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. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S7070 |
GSK J4 HClGSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family. |
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). |
|
| S7237 |
OG-L002OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM in a cell-free assay, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively. |
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.
|
|
| S7281 |
JIB-04JIB-04 is a pan-selective Jumonji histone demethylase inhibitor with IC50 of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D in cell-free assays, respectively. |
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).
|
|
| S7296 |
ML324ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM. |
||
| S7574 |
GSK-LSD1 2HClGSK-LSD1 2HCl is an irreversible, and selective LSD1 inhibitor with IC50 of 16 nM, > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B). |
||
| S5772新 |
AS-8351AS-8351 is a histone demethylase inhibitor that could induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes. |
||
| S7234 |
IOX1IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. |
||
| S7795 |
ORY-1001 (RG-6016) 2HClORY-1001 (RG-6016) 2HCl is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor with IC50 of <20 nM, with high selectivity against related FAD dependent aminoxidases. 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.
|
|
| S7581 |
GSK J1GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, >10-fold selectivity over other tested demethylases. |
||
| S7796 |
GSK2879552 2HClGSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1. |
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.
|
|
| S7680 |
SP2509SP2509 is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. |
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.
|
|
| S8601 |
CP2CP2 is a cyclic peptide that inhibits the JmjC histone demethylases KDM4 with IC50 values of 42 nM and 29 nM for KDM4A and KDM4C, respectively. |
||
| S4800 |
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. |
