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Histone Demethylase
Histone Demethylase Products
- All (28)
- Histone Demethylase Inhibitors (28)
- New Histone Demethylase Products
| Catalog No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| S7070 | GSK J4 HCl | GSK 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. |
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| S7680 | SP2509 | SP2509 (HCI-2509) 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. SP2509 induces apoptosis and promotes autophagy. |
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| S8287 | CPI-455 HCl | CPI-455 HCl is a specific KDM5 inhibitor with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents. | ||
| S7796 | GSK2879552 2HCl | GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1. |
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| S7795 | Iadademstat (ORY-1001) 2HCl | ORY-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. |
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| S7574 | GSK-LSD1 2HCl | GSK-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). | ||
| S7281 | JIB-04 | JIB-04 (NSC 693627) 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. JIB‑04 also induces cell apoptosis. |
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| S7237 | OG-L002 | OG-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. |
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| S7296 | ML324 | ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM. | ||
| S7234 | IOX1 | IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 is an inhibitor of ALKBH5. | ||
| S7581 | GSK J1 | GSK-J1 is a highly potent inhibitor of H3K27 histone demethylase JMJD3 (KDM6B) and UTX (KDM6A) with IC50 of 60 nM in cell-free assays for JMJD3 (KDM6B) , respectively, >10-fold selectivity over other tested demethylases, with IC50 of 0.95μM and 1.76μM towards JARID1B/C. | ||
| S8601 | CP2 | CP2 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. | ||
| S6389 | CPI-455 | CPI-455 is a specific KDM5 inhibitor with an IC50 of 10 nM for full-length KDM5A in enzymatic assays. CPI-455 shows over 200-fold selectivity for KDM5 relative to KDM2, 3, 4, 6, and 7 enzymes. |
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| S1325 | L-2-Hydroxyglutaric acid disodium | L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) is an epigenetic modifier and a putative oncometabolite in kidney cancer that inhibits histone demethylases and hence promotes histone methylation. L-2-Hydroxyglutaric acid disodium is also an inhibitor of mitochondrial creatine kinase (Mi-CK) with Km and Ki of 2.52 mM and 11.13 mM, respectively. |
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| E7827New | KDM5-IN-1 | KDM5-IN-1 is a potent, selective and orally bioavailable inhibitor of KDM5 with an IC50 value of 15.1 nM. It displays an increased cell potency with an EC50 value of 0.34 μM, respectively. | ||
| E0132 | NCGC00244536 | NCGC00244536 is a novel KDM4 Inhibitor with an IC50 of ∼10 nM. |
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| S0269 | GSK467 | GSK467 is a cell penetrant and selective inhibitor of KDM5B (JARID1B/PLU1) with Ki of 10 nM. GSK467 shows apparent 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other JmJ family members. | ||
| E1819New | Zavondemstat | Zavondemstat(QC8222, TACH 101) is a small-molecule pan-inhibitor of histone lysine demethylase 4D (KDM4D) that selectively targets KDM4A-D with no effect on other KDM families. It exhibits potent antiproliferative activity in various cancer cell lines and organoid models. It displays antineoplastic activity and acts as a potential anticancer agent. | ||
| S9882 | PFI-90 | PFI-90 is a selective inhibitor of the histone demethylase KDM3B. PFI-90 induces apoptosis and cell differentiation resulting in delayed tumor progression in vivo. | ||
| E1793New | TC-E5002(KDM2/7-IN-1) | TC-E5002(KDM2/7-IN-1) is a selective inhibitor of histone demethylase KDM2/7 subfamily with IC50s of 6.8, 0.2, and 1.2 µM for KDM2A, KDM7A, and KDM7B, respectively. It is selective for the KDM2/7 subfamily over KDM4A, KDM4C, KDM5A, and KDM6A/UTX with IC50s of >120, 83, 55, and 100 µM, respectively. It exhibits antiproliferative activity, indicating its potential as an anticancer agent. | ||
| S5772 | AS-8351 | AS-8351 is a histone demethylase inhibitor that could induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes. | ||
| S1059 | KDM4D-IN-1 | KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM. | ||
| E4794New | GSK-J4 | GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A that ameliorates experimental autoimmune encephalomyelitis (EAE). It is also an inhibitor of TNF-α production, with an IC50 of 9 μM. It shows potential as a treatment for inflammatory and autoimmune disorders. | ||
| S0356 | Pulrodemstat (CC-90011) besylate | Pulrodemstat (CC-90011) besylate (LSD1-IN-7 benzenesulfonate) is a potent and orally active lysine specific demethylase-1 (LSD1) inhibitor that is found to be effective in various tumors. | ||
| E1733 | PBIT | PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. It inhibits JARID1B (KDM5B/PLU1), JARID1Aand JARID1C with an IC50 of 3 μM, 6 μM and 4.9 μM respectively. It is capable of inhibiting the multiplication of breast cancer cell lines expressing high levels of JARIDB1. | ||
| S0201 | Z-JIB-04 (NSC 693627) | Z-JIB-04 (NSC 693627, JIB-04 Z-isomer) is an isomer of JIB-04. JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50 of 230 nM, 340 nM, 855 nM, 445 nM, 435 nM, 1100 nM and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively. | ||
| S4800New | Daminozide | Daminozide (Aminozide, DMASA, DIMG, B 995, Alar, Kylar, B-NINE, SADH) is a plant growth regulator that selectively inhibits human KDM2/7 histone demethylases, with IC50 of 0.55 μM for PHF8 (KDM7B), 1.5 μM for KDM2A, and 2.1 μM for KIAA1718 (KDM7A). It shows over 100-fold selectivity for the KDM2/7 subfamily compared to other histone demethylase subfamilies, with significantly weaker activity against enzymes such as KDM3A with IC50 of 127 μM. | ||
| S8438 | T-3775440 HCl | T-3775440 HCl is an irreversible LSD1 inhibitor that is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with an IC50 value of 2.1 nmol/L. | ||
| S7070 | GSK J4 HCl | GSK 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. |
|
|
| S7680 | SP2509 | SP2509 (HCI-2509) 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. SP2509 induces apoptosis and promotes autophagy. |
|
|
| S8287 | CPI-455 HCl | CPI-455 HCl is a specific KDM5 inhibitor with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents. | ||
| S7796 | GSK2879552 2HCl | GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1. |
|
|
| S7795 | Iadademstat (ORY-1001) 2HCl | ORY-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. |
|
|
| S7574 | GSK-LSD1 2HCl | GSK-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). | ||
| S7281 | JIB-04 | JIB-04 (NSC 693627) 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. JIB‑04 also induces cell apoptosis. |
|
|
| S7237 | OG-L002 | OG-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. |
|
|
| S7296 | ML324 | ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM. | ||
| S7234 | IOX1 | IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 is an inhibitor of ALKBH5. | ||
| S7581 | GSK J1 | GSK-J1 is a highly potent inhibitor of H3K27 histone demethylase JMJD3 (KDM6B) and UTX (KDM6A) with IC50 of 60 nM in cell-free assays for JMJD3 (KDM6B) , respectively, >10-fold selectivity over other tested demethylases, with IC50 of 0.95μM and 1.76μM towards JARID1B/C. | ||
| S8601 | CP2 | CP2 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. | ||
| S6389 | CPI-455 | CPI-455 is a specific KDM5 inhibitor with an IC50 of 10 nM for full-length KDM5A in enzymatic assays. CPI-455 shows over 200-fold selectivity for KDM5 relative to KDM2, 3, 4, 6, and 7 enzymes. |
||
| S1325 | L-2-Hydroxyglutaric acid disodium | L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) is an epigenetic modifier and a putative oncometabolite in kidney cancer that inhibits histone demethylases and hence promotes histone methylation. L-2-Hydroxyglutaric acid disodium is also an inhibitor of mitochondrial creatine kinase (Mi-CK) with Km and Ki of 2.52 mM and 11.13 mM, respectively. |
||
| E7827New | KDM5-IN-1 | KDM5-IN-1 is a potent, selective and orally bioavailable inhibitor of KDM5 with an IC50 value of 15.1 nM. It displays an increased cell potency with an EC50 value of 0.34 μM, respectively. | ||
| E0132 | NCGC00244536 | NCGC00244536 is a novel KDM4 Inhibitor with an IC50 of ∼10 nM. |
||
| S0269 | GSK467 | GSK467 is a cell penetrant and selective inhibitor of KDM5B (JARID1B/PLU1) with Ki of 10 nM. GSK467 shows apparent 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other JmJ family members. | ||
| E1819New | Zavondemstat | Zavondemstat(QC8222, TACH 101) is a small-molecule pan-inhibitor of histone lysine demethylase 4D (KDM4D) that selectively targets KDM4A-D with no effect on other KDM families. It exhibits potent antiproliferative activity in various cancer cell lines and organoid models. It displays antineoplastic activity and acts as a potential anticancer agent. | ||
| S9882 | PFI-90 | PFI-90 is a selective inhibitor of the histone demethylase KDM3B. PFI-90 induces apoptosis and cell differentiation resulting in delayed tumor progression in vivo. | ||
| E1793New | TC-E5002(KDM2/7-IN-1) | TC-E5002(KDM2/7-IN-1) is a selective inhibitor of histone demethylase KDM2/7 subfamily with IC50s of 6.8, 0.2, and 1.2 µM for KDM2A, KDM7A, and KDM7B, respectively. It is selective for the KDM2/7 subfamily over KDM4A, KDM4C, KDM5A, and KDM6A/UTX with IC50s of >120, 83, 55, and 100 µM, respectively. It exhibits antiproliferative activity, indicating its potential as an anticancer agent. | ||
| S5772 | AS-8351 | AS-8351 is a histone demethylase inhibitor that could induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes. | ||
| S1059 | KDM4D-IN-1 | KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM. | ||
| E4794New | GSK-J4 | GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A that ameliorates experimental autoimmune encephalomyelitis (EAE). It is also an inhibitor of TNF-α production, with an IC50 of 9 μM. It shows potential as a treatment for inflammatory and autoimmune disorders. | ||
| S0356 | Pulrodemstat (CC-90011) besylate | Pulrodemstat (CC-90011) besylate (LSD1-IN-7 benzenesulfonate) is a potent and orally active lysine specific demethylase-1 (LSD1) inhibitor that is found to be effective in various tumors. | ||
| E1733 | PBIT | PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. It inhibits JARID1B (KDM5B/PLU1), JARID1Aand JARID1C with an IC50 of 3 μM, 6 μM and 4.9 μM respectively. It is capable of inhibiting the multiplication of breast cancer cell lines expressing high levels of JARIDB1. | ||
| S0201 | Z-JIB-04 (NSC 693627) | Z-JIB-04 (NSC 693627, JIB-04 Z-isomer) is an isomer of JIB-04. JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50 of 230 nM, 340 nM, 855 nM, 445 nM, 435 nM, 1100 nM and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively. | ||
| S4800New | Daminozide | Daminozide (Aminozide, DMASA, DIMG, B 995, Alar, Kylar, B-NINE, SADH) is a plant growth regulator that selectively inhibits human KDM2/7 histone demethylases, with IC50 of 0.55 μM for PHF8 (KDM7B), 1.5 μM for KDM2A, and 2.1 μM for KIAA1718 (KDM7A). It shows over 100-fold selectivity for the KDM2/7 subfamily compared to other histone demethylase subfamilies, with significantly weaker activity against enzymes such as KDM3A with IC50 of 127 μM. | ||
| S8438 | T-3775440 HCl | T-3775440 HCl is an irreversible LSD1 inhibitor that is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with an IC50 value of 2.1 nmol/L. | ||
| E7827New | KDM5-IN-1 | KDM5-IN-1 is a potent, selective and orally bioavailable inhibitor of KDM5 with an IC50 value of 15.1 nM. It displays an increased cell potency with an EC50 value of 0.34 μM, respectively. | ||
| E1819New | Zavondemstat | Zavondemstat(QC8222, TACH 101) is a small-molecule pan-inhibitor of histone lysine demethylase 4D (KDM4D) that selectively targets KDM4A-D with no effect on other KDM families. It exhibits potent antiproliferative activity in various cancer cell lines and organoid models. It displays antineoplastic activity and acts as a potential anticancer agent. | ||
| E1793New | TC-E5002(KDM2/7-IN-1) | TC-E5002(KDM2/7-IN-1) is a selective inhibitor of histone demethylase KDM2/7 subfamily with IC50s of 6.8, 0.2, and 1.2 µM for KDM2A, KDM7A, and KDM7B, respectively. It is selective for the KDM2/7 subfamily over KDM4A, KDM4C, KDM5A, and KDM6A/UTX with IC50s of >120, 83, 55, and 100 µM, respectively. It exhibits antiproliferative activity, indicating its potential as an anticancer agent. | ||
| E4794New | GSK-J4 | GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A that ameliorates experimental autoimmune encephalomyelitis (EAE). It is also an inhibitor of TNF-α production, with an IC50 of 9 μM. It shows potential as a treatment for inflammatory and autoimmune disorders. | ||
| S4800New | Daminozide | Daminozide (Aminozide, DMASA, DIMG, B 995, Alar, Kylar, B-NINE, SADH) is a plant growth regulator that selectively inhibits human KDM2/7 histone demethylases, with IC50 of 0.55 μM for PHF8 (KDM7B), 1.5 μM for KDM2A, and 2.1 μM for KIAA1718 (KDM7A). It shows over 100-fold selectivity for the KDM2/7 subfamily compared to other histone demethylase subfamilies, with significantly weaker activity against enzymes such as KDM3A with IC50 of 127 μM. |
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Tags: Histone Demethylase inhibitor|Histone Demethylase agonist|Histone Demethylase activator|Histone Demethylase inducer|Histone Demethylase antagonist|Histone Demethylase signaling pathway|Histone Demethylase assay kit
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