LSD1

抑制剂选择性比较

LSD1产品

所有产品 LSD1抑制剂(5)

产品目录	产品描述	文献引用	实验数据
S7237	OG-L002 OG-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。	Clin Cancer Res, 2018, 10.1158/1078-0432 Cell Death Dis, 2018, 9(10):1038 Oncotarget, 2018, 9(5):6450-6462	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 2HCl GSK-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。	Epigenetics, 2018, 13(5):557-572
S7795	ORY-1001 (RG-6016) 2HCl ORY-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。	Genes Dev, 2019, 33(23-24):1718-1738 Cell Death Dis, 2017, 8(2):e2631	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.
S7796	GSK2879552 2HCl GSK2879552 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。	Front Oncol, 2019, 0.87569444444 Pigment Cell Melanoma Res, 2019, 10.1111/pcmr.12849 Oncotarget, 2018, 9(5):6450-6462	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	SP2509 SP2509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。	Front Genet, 2019, 10:422 Biochem Biophys Res Commun, 2019, 512(4):852-858 Mol Cancer Res, 2018, 16(10):1458-1469	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.

产品目录	产品描述	文献引用	实验数据
S7237	OG-L002 OG-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。	Clin Cancer Res,2018, 10.1158/1078-0432 Cell Death Dis,2018, 9(10):1038 Oncotarget,2018, 9(5):6450-6462	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 2HCl GSK-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。	Epigenetics,2018, 13(5):557-572
S7795	ORY-1001 (RG-6016) 2HCl ORY-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。	Genes Dev,2019, 33(23-24):1718-1738 Cell Death Dis,2017, 8(2):e2631	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.
S7796	GSK2879552 2HCl GSK2879552 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。	Front Oncol,2019, 0.87569444444 Pigment Cell Melanoma Res,2019, 10.1111/pcmr.12849 Oncotarget,2018, 9(5):6450-6462	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	SP2509 SP2509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。	Front Genet,2019, 10:422 Biochem Biophys Res Commun,2019, 512(4):852-858 Mol Cancer Res,2018, 16(10):1458-1469	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.

Tags: LSD1 inhibitor | LSD1 modulator | LSD1 chemical