- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|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|
|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 Inhibitors (12)
- New Histone Demethylase Products
|Catalog No.||Information||Product Use Citations||Product Validations|
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.
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.