Histone Demethylase

特异性亚型抑制剂

• KDM1 Selective
• KDM2 Selective
• KDM3 Selective
• KDM4 Selective
• KDM5 Selective
• KDM6 Selective

Histone Demethylase产品

目录号	产品描述	文献引用	实验数据
S7070	GSK J4 HCl (GSKJ4 HCl) GSK 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。	Nat Immunol, 2022, 23(3):431-445 Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Cell Death Dis, 2022, 13(2):174	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-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。	Sci Rep, 2021, 11(1):10285 Nat Genet, 2020, 52(10):1011-1017 Sci Rep, 2020, 10(1):377	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.
S7281	JIB-04 JIB-04 (NSC 693627)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。JIB‑04还可诱导细胞凋亡。	mBio, 2022, 13(1):e0337721 Cancer Biol Ther, 2022, 23(1):65-75 Mol Ther Oncolytics, 2021, 20:583-595	G, Western blot analyses to monitor the amount of H3K9me3 in the presence of rhein and MMS (upper panel) and under thetreatment of JIB-04 (lower panel).
S7296	ML324 ML324是一种选择性的jumonji histone demethylase (JMJD2)抑制剂， 其对JMJD2E的IC50为920 nM。	Cancer Biol Ther, 2022, 23(1):65-75 Chem Biol Interact, 2022, 353:109806 Br J Cancer, 2021, 10.1038/s41416-021-01441-7
E0132New	NCGC00244536 NCGC00244536 是一种新型 KDM4 抑制剂，IC50 约为 10 nM。
S6389New	CPI-455 CPI-455 是一种特异性的 KDM5 抑制剂，在酶促测定中对全长 KDM5A 的半数最大抑制浓度 (IC50) 为 10 nM。CPI-455 对 KDM5 的选择性比 KDM2、3、4、6 和 7 酶高 200 倍以上。	Cancers (Basel), 2022, 14(6)1537
S9882New	PFI-90 PFI-90 是组蛋白去甲基化酶KDM3B的选择性抑制剂。PFI-90诱导细胞凋亡和细胞分化，导致体内肿瘤进展延迟。
S0269	GSK467 GSK467 是一种具有细胞渗透性和选择性的 KDM5B (JARID1B/PLU1) 的抑制剂，Ki值为10 nM。GSK467 对KDM4C表现出明显的180倍的选择性，而对KDM6或其他JmJ家族成员没有明显的抑制作用。
S8287	CPI-455 HCl CPI-455 HCl 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。	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Oncogene, 2022, 10.1038/s41388-022-02185-1 Cancers (Basel), 2022, 14(6)1537
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。	Theranostics, 2022, 12(4):1500-1517 J Int Med Res, 2022, 50(1):3000605211067921 Cell Res, 2021, 1-13
S7234	IOX1 IOX1 是2OG oxygenases强效的广谱抑制剂, 包括JmjC demethylases。	Nat Commun, 2022, 13(1):1172 Chem Biol Drug Des, 2022, 10.1111/cbdd.14051 Sci Rep, 2021, 11(1):2942
S7795	Iadademstat (ORY-1001) 2HCl Iadademstat 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。	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Mol Psychiatry, 2022, 10.1038/s41380-022-01508-8 FASEB J, 2022, 36(1):e22122	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.
S5772	AS-8351 AS-8351是组蛋白去甲基化酶（histone demethylase）抑制剂，能够诱导人胚肺成纤维细胞向功能性心肌细胞的重编程过程。
S1059	KDM4D-IN-1 KDM4D-IN-1是有效的KDM4D抑制剂,IC50值为0.41μM。
S7581	GSK J1 GSK-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。	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Front Cell Dev Biol, 2021, 9:702462 Leukemia, 2021, 10.1038/s41375-021-01121-8
S0356	Pulrodemstat (CC-90011) besylate Pulrodemstat (CC-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 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。	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Mol Cell, 2021, S1097-2765(21)01037-6 J Neurosci, 2021, JN-RM-3102-20	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 (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。	Biomedicines, 2022, 10(3)638 Invest Ophthalmol Vis Sci, 2022, 63(3):20 Cell Death Dis, 2021, 12(11):993	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	CP2 CP2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。	Front Cell Dev Biol, 2021, 9:697614 Exp Cell Res, 2021, S0014-4827(21)00315-3 Int Immunopharmacol, 2020, 1;83:106438
S0201	Z-JIB-04 (NSC 693627) Z-JIB-04 (NSC 693627, JIB-04 Z-isomer)是JIB-04的异构体。JIB-04 是一种泛选择性的 Jumonji histone demethylase 抑制剂，对于JARID1A、JMJD2E、JMJD3、JMJD2A、JMJD2B、JMJD2C和JMJD2D的IC50值分别为230 nM、340 nM、855 nM、445 nM、435 nM、1100 nM和290 nM。
S4800	Daminozide Daminozide (Aminozide, DMASA, DIMG, B 995, Alar，Kylar，B-NINE, SADH), 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.
S1325	L-2-Hydroxyglutaric acid disodium L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) 是一种表观遗传修饰剂和在肾脏癌中推测的肿瘤代谢物，抑制 histone demethylases，因此促进组蛋白甲基化。L-2-Hydroxyglutaric acid disodium 也是一种 mitochondrial creatine kinase (Mi-CK) 的抑制剂，对应的Km值和Ki值分别为2.52 mM和11.13 mM。
S8438	T-3775440 HCl T-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
S7070	GSK J4 HCl (GSKJ4 HCl) GSK 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。	Nat Immunol,2022, 23(3):431-445 Nat Chem Biol,2022, 10.1038/s41589-022-00996-7 Cell Death Dis,2022, 13(2):174	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-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。	Sci Rep,2021, 11(1):10285 Nat Genet,2020, 52(10):1011-1017 Sci Rep,2020, 10(1):377	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.
S7281	JIB-04 JIB-04 (NSC 693627)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。JIB‑04还可诱导细胞凋亡。	mBio,2022, 13(1):e0337721 Cancer Biol Ther,2022, 23(1):65-75 Mol Ther Oncolytics,2021, 20:583-595	G, Western blot analyses to monitor the amount of H3K9me3 in the presence of rhein and MMS (upper panel) and under thetreatment of JIB-04 (lower panel).
S7296	ML324 ML324是一种选择性的jumonji histone demethylase (JMJD2)抑制剂， 其对JMJD2E的IC50为920 nM。	Cancer Biol Ther,2022, 23(1):65-75 Chem Biol Interact,2022, 353:109806 Br J Cancer,2021, 10.1038/s41416-021-01441-7
E0132New	NCGC00244536 NCGC00244536 是一种新型 KDM4 抑制剂，IC50 约为 10 nM。
S6389New	CPI-455 CPI-455 是一种特异性的 KDM5 抑制剂，在酶促测定中对全长 KDM5A 的半数最大抑制浓度 (IC50) 为 10 nM。CPI-455 对 KDM5 的选择性比 KDM2、3、4、6 和 7 酶高 200 倍以上。	Cancers (Basel),2022, 14(6)1537
S9882New	PFI-90 PFI-90 是组蛋白去甲基化酶KDM3B的选择性抑制剂。PFI-90诱导细胞凋亡和细胞分化，导致体内肿瘤进展延迟。
S0269	GSK467 GSK467 是一种具有细胞渗透性和选择性的 KDM5B (JARID1B/PLU1) 的抑制剂，Ki值为10 nM。GSK467 对KDM4C表现出明显的180倍的选择性，而对KDM6或其他JmJ家族成员没有明显的抑制作用。
S8287	CPI-455 HCl CPI-455 HCl 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。	Nat Chem Biol,2022, 10.1038/s41589-022-00996-7 Oncogene,2022, 10.1038/s41388-022-02185-1 Cancers (Basel),2022, 14(6)1537
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。	Theranostics,2022, 12(4):1500-1517 J Int Med Res,2022, 50(1):3000605211067921 Cell Res,2021, 1-13
S7234	IOX1 IOX1 是2OG oxygenases强效的广谱抑制剂, 包括JmjC demethylases。	Nat Commun,2022, 13(1):1172 Chem Biol Drug Des,2022, 10.1111/cbdd.14051 Sci Rep,2021, 11(1):2942
S7795	Iadademstat (ORY-1001) 2HCl Iadademstat 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。	Nat Chem Biol,2022, 10.1038/s41589-022-00996-7 Mol Psychiatry,2022, 10.1038/s41380-022-01508-8 FASEB J,2022, 36(1):e22122	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.
S5772	AS-8351 AS-8351是组蛋白去甲基化酶（histone demethylase）抑制剂，能够诱导人胚肺成纤维细胞向功能性心肌细胞的重编程过程。
S1059	KDM4D-IN-1 KDM4D-IN-1是有效的KDM4D抑制剂,IC50值为0.41μM。
S7581	GSK J1 GSK-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。	Nat Chem Biol,2022, 10.1038/s41589-022-00996-7 Front Cell Dev Biol,2021, 9:702462 Leukemia,2021, 10.1038/s41375-021-01121-8
S0356	Pulrodemstat (CC-90011) besylate Pulrodemstat (CC-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 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。	Nat Chem Biol,2022, 10.1038/s41589-022-00996-7 Mol Cell,2021, S1097-2765(21)01037-6 J Neurosci,2021, JN-RM-3102-20	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 (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。	Biomedicines,2022, 10(3)638 Invest Ophthalmol Vis Sci,2022, 63(3):20 Cell Death Dis,2021, 12(11):993	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	CP2 CP2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。	Front Cell Dev Biol,2021, 9:697614 Exp Cell Res,2021, S0014-4827(21)00315-3 Int Immunopharmacol,2020, 1;83:106438
S0201	Z-JIB-04 (NSC 693627) Z-JIB-04 (NSC 693627, JIB-04 Z-isomer)是JIB-04的异构体。JIB-04 是一种泛选择性的 Jumonji histone demethylase 抑制剂，对于JARID1A、JMJD2E、JMJD3、JMJD2A、JMJD2B、JMJD2C和JMJD2D的IC50值分别为230 nM、340 nM、855 nM、445 nM、435 nM、1100 nM和290 nM。
S4800	Daminozide Daminozide (Aminozide, DMASA, DIMG, B 995, Alar，Kylar，B-NINE, SADH), 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.
S1325	L-2-Hydroxyglutaric acid disodium L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) 是一种表观遗传修饰剂和在肾脏癌中推测的肿瘤代谢物，抑制 histone demethylases，因此促进组蛋白甲基化。L-2-Hydroxyglutaric acid disodium 也是一种 mitochondrial creatine kinase (Mi-CK) 的抑制剂，对应的Km值和Ki值分别为2.52 mM和11.13 mM。
S8438	T-3775440 HCl T-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。