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

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S7070 GSK J4 HCl (GSKJ4 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
S0269 GSK467 ˂1 mg/mL 8 mg/mL ˂1 mg/mL
S0201 Z-JIB-04 (NSC 693627) <1 mg/mL 8 mg/mL '''''<1 mg/mL
S1059 KDM4D-IN-1 <1 mg/mL 6 mg/mL <1 mg/mL
S8287 CPI-455 HCl <1 mg/mL 10 mg/mL 2 mg/mL
S7574 GSK-LSD1 2HCl 57 mg/mL 57 mg/mL -1 mg/mL
S7234 IOX1 <1 mg/mL 37 mg/mL <1 mg/mL
S7795 Iadademstat (ORY-1001) 2HCl 61 mg/mL 5 mg/mL '4 mg/mL
S5772 AS-8351 <1 mg/mL 58 mg/mL <1 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
S8438 T-3775440 HCl 22 mg/mL 69 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 HCl (GSKJ4 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.

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.

S7281

JIB-04

JIB-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. JIB‑04 also induces cell apoptosis.

S7296

ML324

ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 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.

S0201

Z-JIB-04 (NSC 693627)

Z-JIB-04 (NSC 693627) 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.

S1059

KDM4D-IN-1

KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM.

S8287

CPI-455 HCl

CPI-455 is a specific KDM5 inhibitor, 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.

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).

S7234

IOX1

IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases.

S7795

Iadademstat (ORY-1001) 2HCl

Iadademstat 2HCl (ORY-1001, RG-6016) 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.

S5772

AS-8351

AS-8351 is a histone demethylase inhibitor that could induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.

S7581

GSK J1

GSK-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 2HCl

GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1.

S7680

SP2509

SP2509 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.

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.

S4800

Daminozide

Daminozide, 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.

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.

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 HCl (GSKJ4 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.

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.

S7281

JIB-04

JIB-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. JIB‑04 also induces cell apoptosis.

S7296

ML324

ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 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.

S0201

Z-JIB-04 (NSC 693627)

Z-JIB-04 (NSC 693627) 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.

S1059

KDM4D-IN-1

KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM.

S8287

CPI-455 HCl

CPI-455 is a specific KDM5 inhibitor, 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.

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).

S7234

IOX1

IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases.

S7795

Iadademstat (ORY-1001) 2HCl

Iadademstat 2HCl (ORY-1001, RG-6016) 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.

S5772

AS-8351

AS-8351 is a histone demethylase inhibitor that could induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.

S7581

GSK J1

GSK-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 2HCl

GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1.

S7680

SP2509

SP2509 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.

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.

S4800

Daminozide

Daminozide, 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.

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.