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
  • 溶解度
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 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
S7574 GSK-LSD1 2HCl 57 mg/mL 57 mg/mL -1 mg/mL
S4800 Daminozide -1 mg/mL 32 mg/mL -1 mg/mL
S8601 CP2 100 mg/mL -1 mg/mL -1 mg/mL
S7234 IOX1 <1 mg/mL 37 mg/mL <1 mg/mL
S7795 ORY-1001 (RG-6016) 2HCl 61 mg/mL 5 mg/mL 4 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
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

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.

S7296

ML324

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

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).

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.

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.

S7234

IOX1

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

S7795

ORY-1001 (RG-6016) 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.

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.