LSD1
抑制剂选择性比较
LSD1产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| 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。 |
Nalm6 cells were first treated with JIB-04 at 0.5 μM, OG-L002 at 10 μM or DMSO for 4 h, then 100 nM of dex or ethanol was added to the media for an additional 20 h. Lysates were analyzed by immunoblot with the indicated antibodies. Results shown are representative of three independent experiments.
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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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| S7795 |
Iadademstat (ORY-1001) 2HClIadademstat 2HCl (ORY-1001, RG-6016) 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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| S6722 |
Seclidemstat (SP-2577)Seclidemstat (SP-2577) 是一种有效的、口服的、可生物利用的 lysine-specific demethylase 1 (LSD1/KDM1A) 的抑制剂，IC50值为127 nM。 Seclidemstat（SP-2577）具有潜在的抗肿瘤活性。 |
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| S0356 |
CC-90011 besylateCC-90011 besylate (LSD1-IN-7 benzenesulfonate) 是一种有效的口服活性 lysine specific demethylase-1 (LSD1) 抑制剂，并被发现在多种肿瘤治疗中有效。 |
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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 (HCI-2509)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。SP2509 可诱导凋亡并促进自噬。 |
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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| S8438 |
T-3775440 HClT-3775440 HCl是一种不可逆的LSD1抑制剂。相对于其他单胺氧化酶，它对LSD1具有高选择性，IC50为2.1 nM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| 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。 |
Nalm6 cells were first treated with JIB-04 at 0.5 μM, OG-L002 at 10 μM or DMSO for 4 h, then 100 nM of dex or ethanol was added to the media for an additional 20 h. Lysates were analyzed by immunoblot with the indicated antibodies. Results shown are representative of three independent experiments.
|
|
| 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。 |
||
| S7795 |
Iadademstat (ORY-1001) 2HClIadademstat 2HCl (ORY-1001, RG-6016) 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.
|
|
| S6722 |
Seclidemstat (SP-2577)Seclidemstat (SP-2577) 是一种有效的、口服的、可生物利用的 lysine-specific demethylase 1 (LSD1/KDM1A) 的抑制剂，IC50值为127 nM。 Seclidemstat（SP-2577）具有潜在的抗肿瘤活性。 |
||
| S0356 |
CC-90011 besylateCC-90011 besylate (LSD1-IN-7 benzenesulfonate) 是一种有效的口服活性 lysine specific demethylase-1 (LSD1) 抑制剂，并被发现在多种肿瘤治疗中有效。 |
||
| 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 (HCI-2509)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。SP2509 可诱导凋亡并促进自噬。 |
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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| S8438 |
T-3775440 HClT-3775440 HCl是一种不可逆的LSD1抑制剂。相对于其他单胺氧化酶，它对LSD1具有高选择性，IC50为2.1 nM。 |
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