ヒストン脱メチル化酵素 (Histone Demethylase)
|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|
|S8287||CPI-455 HCl||<1 mg/mL||10 mg/mL||2 mg/mL|
|S8601||CP2||100 mg/mL||-1 mg/mL||-1 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||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|
- Histone Demethylase阻害剤(13)
- 新Histone Demethylase製品
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.
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).
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.
Hepa1c1c7 cells were seeded in 6 well plates. The following day, cells were treated with either 100 nM of Dex for 1 hours, 5mM of VPA for 2 hours, the respective LSD1 inhibitor, or a combination. In terms of LSD1 inhibitor treatment, cells were dosed with 50 uM (Ampd3) or 100 uM (Hbegf) of OG-L002 for 24 hours. Cells were then harvested, and isolated RNA underwent RT-qPCR using intron-exon primers to measure expression of nascent transcripts. For each of the LSD1 inhibitors used, a representative GR activated (Ampd3) and repressed (Hbegf) gene was analyzed. Error bars represent SEM. Statistical analysis using a paired t test was performed, but none of the results demonstrated significance.
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.
G, Western blot analyses to monitor the amount of H3K9me3 in the presence of rhein and MMS (upper panel) and under the treatment of JIB-04 (lower panel).
ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM.
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.
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.
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.
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).
IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases.
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.
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.
GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1.
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.